novel targets, better treatments - jefferies group · summary up to w24” “filgotinib: promising...

Novel targets, better treatments

Investor Presentation | June 2019

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Disclaimer This presentation contains forward-looking statements, including (without limitation) statements concerning the progress of our clinicalpipeline, the slides captioned “We go step by step on commercial” “Prolific late stage pipeline” “R&D ambition” “Filgotinib program” “FINCHsummary up to w24” “Filgotinib: promising profile” “Inflammation market ~$65B by 2027” “$2.1B market with large unmet needs” “We arebuilding a fibrosis portfolio” “Phase 3 program ISABELA 1&2” “PINTA Phase 2 in IPF” “ROCCELLA Phase 2b trial” “Toledo in inflammation”“Promising preclinical results” “Our Toledo development strategy” “Partnerships” “Solid cash position” “Expected news in 2019”, statementsregarding the expected timing, design and readouts of ongoing and planned clinical trials (i) with filgotinib in RA, IBD, and other potentialindications (ii) with GLPG1690 and GLPG1205 in IPF and Ssc, (iii) with the Toledo program, (iv) with GLPG1972 in OA, (v) with MOR106 inatopic dermatitis and other potential indications, and expectations regarding the commercial potential of our product candidates. Whenused in this presentation, the words “anticipate,” “believe,” “can,” “could,” “estimate,” “expect,” “intend,” “is designed to,” “may,” “might,”“will,” “plan,” “potential,” “possible,” “predict,” “objective,” “should,” and similar expressions are intended to identify forward-lookingstatements.Forward-looking statements involve known and unknown risks, uncertainties and other factors which might cause the actual results,financial condition, performance or achievements of Galapagos, or industry results, to be materially different from any future results,financial conditions, performance or achievements expressed or implied by such forward-looking statements. Among the factors that mayresult in differences are the inherent uncertainties associated with competitive developments, clinical trial and product developmentactivities, regulatory approval requirements (including that data from the company's development programs may not support registrationor further development of its compounds due to safety, efficacy or other reasons), reliance on third parties (including Galapagos’collaboration partners Gilead, Servier, MorphoSys, and Novartis) and estimating the commercial potential of its product candidates. Afurther list and description of these risks, uncertainties and other risks can be found in Galapagos’ Securities and Exchange Commission(“SEC”) filing and reports, including Galapagos’ most recent Form 20-F and subsequent filings with the SEC. Given these uncertainties,you are advised not to place any undue reliance on such forward-looking statements.All statements herein speak only as of the release date of this document. Galapagos expressly disclaims any obligation to update anystatement in this document to reflect any change in future development with respect thereto, any future results, or any change in events,conditions and/or circumstances, on which any statement is based, unless specifically required by law or regulation.Under no circumstances may any copy of this presentation, if obtained, be retained, copied, or transmitted.

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We discover novel targets

balanced unbalanced

4

Prolific late stage pipeline area preclinical phase 1 phase 2 phase 3

filgotinib

IPF/fibrosis

OA

AtD

inflammation fibrosis

In Ph3 and Ph2, proprietary

10+ indications, more Ph2 readouts in ‘19

Ph2 underway

>20 programs

Ph2b underway

>40 clinical trials planned in 2019

5

We go step by step on commercial

GLPG1690 IPFglobal scale, independent launch

collaborations as opportunity

filgotinibhome territorybooking sales

filgotinibtop EU markets

Gilead co-promotion

2021EU - IBD

2022+ US & prioritized ROW

2020Benelux –RA

Mission:established global biopharma

Note: filgotinib and GLPG1690 are investigational drugs and there is no guarantee they will be approved

6

Filgotinib programarea phase 1 phase 2 phase 3 status

rheumatoid arthritis recruited

ulcerative colitis recruited

Crohn’s disease recruiting

psoriatic arthritis study completed

ankylosing spondylitis study completed

small bowel CD recruiting

fistulizing CD recruiting

Sjögren’s recruited

cutaneous lupus recruited

lupus nephropathy recruited

uveitis recruiting

7

Phase 3 FINCH program in RA100 and 200 mg

FINCH 1: MTX - IR ACR20 at W12MTX add-onadalimumab controlradiographic assessment

1,759 52 weeks

449 24 weeks ACR20 at W12cDMARD add-on

FINCH 3: MTX naïve 1,252 52 weeks ACR20 at W24monotherapy, +MTX armsradiographic assessment

FINCH 2: biologic - IR

8

76.6

47.2

26.3

69.8

36.3

18.5

70.8

35.1

14.2

49.9

19.8

6.7

0

20

40

60

80

100

ACR20 responders (% subjects) ACR50 responders (% subjects) ACR70 responders (% subjects)

FIL 200 mg + MTX FIL 100 mg + MTX ADA 40 mg + MTX PBO + MTX

ACR20/50/70

FIL: filgotinib; ADA: adalimumab; MTX: methotrexate; PBO: placeboNote: MTX-IR population (inadequate response to MTX); all arms were on a stable dose of MTXPress release. Gilead Sciences, Inc. and Galapagos NV. March 28, 2019

W12Δ 26.7%p < 0.001

Δ 19.9%p < 0.001

Δ 27.4%p < 0.001

Δ 16.5%p < 0.001 Δ 19.6%

p < 0.001

Δ 11.8%p < 0.001

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LDA & clinical remissionW12

49.7*

33.9#†38.8

23.8**†

43.4

23.723.4

9.3

0

20

40

60

80

100

LDA - DAS28(CRP) ≤3.2 (% subjects) Remission - DAS28(CRP) ≤2.6 (% subjects)


*p

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Radiographic progressionW24

FIL: filgotinib; ADA: adalimumab; MTX: methotrexate; PBO: placebo; mTSS: modified total Sharp scoresNote: MTX-IR population (inadequate response to MTX); all arms were on a stable dose of MTX

0.13

0.17 0.16

0.38

0

0.1

0.2

0.3

0.4

0.5


Mea

n m

TSS

chan

ge fr

om b

asel

ine

Δ -0.28; p < 0.001

Δ -0.26; p < 0.001

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FINCH safety data week 24Low incidence of DVT & infections

No (%)PBO/MTX filgotinibtotal

N=1039 N=2088

serious infection 10 (1.0) 29 (1.4)

herpes zoster 4 (0.4) 12 (0.6)

DVT/PE 3 (0.3) 1 (

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Long term safety data

event per

100 PYE

filgotinib

50-200 mg

DARWIN 3 week 156

patient year exp. 2,203

serious infection 1.2

herpes zoster 1.5

DVT/PE 2/2,203*0.1

deaths 0.2

Data on file; DVT/PE = deep venous thrombosis/pulmonary embolism* one single patient experiencing DVT and PE

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Filgotinib: exciting profile

SAFETY DATA>3,000 PYEexcellent safety profile continues

EFFICACY DATAclinically meaningful responsesrapid onsetsustained responsestrong in patient outcomes

CONVENIENCEonce-daily oral2 doses flexibility

Potentially best-in-class in multiple indications

Note: filgotinib is a compound in development by Gilead and Galapagos. The profile described data above was derived from the filgotinib DARWIN and FINCH studies.

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Inflammation market $65B by 2027

RA~30

CD~10

UC~9

AS~8

PsA~10

estimated market size, $B

Source: Goldman Sachs 2017, Leerink 2017, Stifel 2017, Global Data, Galapagos estimates

non-RA indications 60% of future marketfilgotinib possibly 1st or 2nd JAKi in most indications

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Germany – JAKi’s challenging aTNFs

Source: IQVia, only aTNF and JAKi molecules represented

Q1 Q2 Q3 Q4 Q1 Q2 Q3 Q4 Q1 Q2 Q3

2016 2017 2018

Q4

Humira & biosimilars

Enbrel & biosimilars

Roactemra-3.8%

-7.2%

-2.3%

6.7%

10.1%

35%

30%

20%

10%

25%

15%

5%

0%

Xeljanz

Olumiant

MS change Q4-18 vs Q4-16

16

‘1690 for idiopathic pulmonary fibrosis (IPF)

Progressive lung fibrosis leading to death

• 200k cases in US & EU• 75k new cases every

year• Median survival 2-5 years

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IPF $2.1B market with large unmet needs

2018 drug sales: $2.1B

nintedanib & pirfenidonehave limitations• slow FVC decline• poor tolerability for patients• ~25% annual discontinuations

pirfenidone nintedanib

Sources: Global Data, Maher et al. BMC Pulmonary Medicine (2017) 17:124, sales figures from Roche (pirfenidone; Esbriet®) and Boehringer Ingelheim (nintedanib; Ofev®)Note: FVC = Forced vital capacity

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program discovery preclinical Ph1 Ph2 Ph3

‘1690 (autotaxin) ISABELA IPF

‘1205 (GPR84) PINTA IPF

New IPF programs

‘1690 NOVESA SSc

We are building a fibrosis portfolio

• Opportunity to combine• Several fibrosis programs in discovery

Status end ‘18

Status end ’19 (projected)

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Phase 3 program ISABELA 1&2

Topline Part 1 expected Q3 ‘18‘1690 600mg

placebo

At least 52 weeks

screening follow-up

‘1690 200mg

• 1500 IPF patients total in two identical Phase 3 studies• Patients remain on standard of care throughout• Global program with US & EU component• Primary endpoint: FVC decline at 52 weeks• Secondary: hospitalizations, mortality, quality of life, safety/tolerability

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‘1972for osteoarthritis (OA)

Breakdown of joint cartilage• 118M patients in US, Europe

& Japan• No disease-modifying drugs

21

‘1972 low dose

‘1972 medium dose

‘1972 high dose

vehicle

‘1972 protects cartilageHistopathology in mouse model

cartilage

Source: Amantini et al OARSI 2018

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Reduction of ARGS‘1972 Phase 1b study in OA patients

Dose-dependent reduction of ARGS, well-tolerated in OA patients

seru

m A

RG

S %

redu

ctio

n vs

bas

elin

e

high dose

med dose

low dose

placebo

days post dosing

Chart1

placebo03.05616172116967283.95622520632767753.41444426136847272.831315773442854212.7224337294368743.9832277527313665.94521999191763056.86257265277048936.593731228873279403.05616172116967283.95622520632767753.41444426136847272.831315773442854212.7224337294368743.9832277527313665.94521999191763056.86257265277048936.593731228873279413681015222943500-1.6957180439390573-2.4290106719463034-1.3691246631411336-3.94847948897045388.4265120170106176-5.8613724112783432-3.64013113050866850.975435624579449214.1576099731943144‘1972 dose 102.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877802.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.0891799183487781368101522294350011.88718306020534925.8115035223457629.41407918071999836.26708932022290839.62279814820996639.93763308496654938.432978092255723-5.7636619126092885-6.4729351895266554‘1972 dose 202.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781102.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.633479450907811136810152229435003.706339638082214421.4840962812108132.66887652175267938.37521256537915845.85912944049331945.7036166259120944.927042591134409-12.689923154782715-14.380494797641056‘1972 dose 302.28481036718146812.40992799782371942.47819750042884123.01773941105111732.84339852029234042.71718102276922174.47066463189533622.84388318194113143.914163047530318202.28481036718146812.40992799782371942.47819750042884123.01773941105111732.84339852029234042.71718102276922174.47066463189533622.84388318194113143.91416304753031821368101522294350012.7874555796888828.66601706390963939.91722411634599943.03256863984385253.48692930965581453.95655175943095150.429061712309981-6.3471478344633647-11.587607986329798

days post-dosing

ARGS % reduction vs baseline

Blad1

STUDYIDTUBEIDSUBJIDPERIODDAYHOUR_NOMINALANALYTECONCENTRATIONCONCENTRATION_UNITSBIOLOGICAL_MATRIXLABORATORYComment

GLPG1972-CL-104001-003 D1 pre-dose001-003110aggrecan ARGS neoepitope0.109pmol/mLSerumAndré Struglics research groupBackup sample








GLPG1972-CL-104001-003 D43 FU001-0031430aggrecan ARGS neoepitope0.084pmol/mLSerumAndré Struglics research groupBackup sample


GLPG1972-CL-104001-009 D1 pre-dose001-009110aggrecan ARGS neoepitope0.100pmol/mLSerumAndré Struglics research group


GLPG1972-CL-104001-009 D6 pre-dose001-009160aggrecan ARGS neoepitope0.071pmol/mLSerumAndré Struglics research groupValue based on single well analysis due to low volume of sample.






GLPG1972-CL-104001-009 D43 FU001-0091430aggrecan ARGS neoepitope0.115pmol/mLSerumAndré Struglics research group

GLPG1972-CL-104001-009 D50 FU001-0091500aggrecan ARGS neoepitope0.098pmol/mLSerumAndré Struglics research groupAnalysed on a seperate plate, thusly not on the same plate as the other primary samples of this subject.







































































































































































GLPG1972-CL-104001-052 EDV001-0521N/AN/Aaggrecan ARGS neoepitope0.079pmol/mLSerumAndré Struglics research group

GPLG1972-CL-104001-053 D1 pre-dose001-053110aggrecan ARGS neoepitope0.201pmol/mLSerumAndré Struglics research group








GPLG1972-CL-104001-053 D43 FU001-0531430aggrecan ARGS neoepitope0.214pmol/mLSerumAndré Struglics research group






































































































#LN00122

The SAS System

Unique Subject IdentifierRandomization numbergroupUnique Subject IdentifierRandomization numbergroup

GLPG1972-CL-104-001-009101100mgGLPG1972-CL-104-001-003103Placebo


GLPG1972-CL-104-001-003103PlaceboGLPG1972-CL-104-001-031203Placebo




GLPG1972-CL-104-001-026107100mg

GLPG1972-CL-104-001-025108PlaceboGLPG1972-CL-104-001-009101100mg

GLPG1972-CL-104-001-028109100mgGLPG1972-CL-104-001-011106100mg







GLPG1972-CL-104-001-045206300mg









GLPG1972-CL-104-001-053305200mg






GLPG1972-CL-104-001-045206300mg

GLPG1972-CL-104-001-049209300mg

GLPG1972-CL-104-001-052210300mg

CL104_placebo

randomization number103108203207302306

Visit IDDay001-003001-025001-031001-048001-067001-073meansemCV%

serum-ARGS (pmol/ml)D1 pre-dose10.1090.1790.0920.0990.1380.1570.1290.01426.96

D3 pre-dose30.1020.1850.0980.1100.1410.1450.1300.01425.56

D6 pre-dose60.1060.1680.0910.1130.1590.1500.1310.01324.31

D8 pre-dose80.0980.1760.0950.1080.1530.1520.1300.01426.41

D10 pre-dose100.1070.1750.0930.1030.1580.1710.1340.01527.96

D15 pre-dose150.0350.1750.0930.1170.1210.1750.1200.02244.39

D22 pre-dose220.1080.1930.0860.1210.1460.1680.1370.01628.90

D29 pre-dose290.1020.1950.0780.1250.1370.1720.1350.01832.35

D43 FU43 FU0.0840.1760.0760.1180.1410.1800.1290.01834.34

D50 FU50 FU0.0820.1690.0750.1180.1450.1550.1240.01631.33

% reductionD1 pre-dose10000000.000.00ERROR:#DIV/0!

D3 pre-dose36.51-3.28-6.70-11.67-2.567.53-1.703.06-441.47

D6 pre-dose62.716.091.52-14.18-15.354.64-2.433.96-398.96

D8 pre-dose810.841.46-3.50-9.20-11.453.64-1.373.41-610.88

D10 pre-dose102.662.31-0.57-4.39-15.10-8.60-3.952.83-175.64

D15 pre-dose1568.222.15-1.63-18.6711.90-11.428.4312.72369.83

D22 pre-dose221.52-7.766.09-22.43-5.94-6.64-5.863.98-166.46

D29 pre-dose296.88-8.9715.50-26.070.42-9.60-3.645.95-400.06

D43 FU43 FU22.971.8017.32-19.46-2.55-14.230.986.861723.31

D50 FU50 FU24.765.8018.30-19.81-5.631.524.166.59388.48

001-00313681015222943 FU50 FU0.10941145794281150.10228659767458650.106450782224346019.754797421165684E-20.10650436978765853.4769939914737397E-20.10775052798615750.10188364119458018.4275432305949999E-28.2317705920089607E-2001-02513681015222943 FU50 FU0.17907705414343450.1849578770666010.16817189922473050.176464425657222010.174934721207234020.17521850424772650.19297223395015450.195139530140804510.17585477604263250.16868317283824752001-03113681015222943 FU50 FU9.1988763728526352E-29.8156119348370499E-29.0586767456228401E-29.521052668952755E-29.2510627615457058E-29.3484372344739497E-28.6389227564847251E-27.7730747824966695E-27.6059409094139191E-27.5156338795829891E-2001-04813681015222943 FU50 FU9.8758197267193953E-20.11028089538827850.112763809630653990.10784184641893550.103098115079321960.11719669960419550.12091037655150250.12450091405895650.1179771230910860.11831775320969301001-06713681015222943 FU50 FU0.137625883312351980.141144561310742990.1587503900615580.153389910380569480.15841081671279950.12125288184736750.145805443591310510.137051117325572010.141133000550446970.14537894352212549001-07313681015222943 FU50 FU0.157294258198367510.145455635884215510.150000300151990010.151572231860170990.170816479381079990.17525267388717350.167738760722637490.172398337192826490.179674657046150490.15490507059421749

Days post-dosing

ARGS level (pmol/mL)

001-00313681015222943 FU50 FU06.51198732033084582.706001523179608610.8429994026362522.657023505410663268.2209335580635641.51805851771224816.88028190993134122.97385128530132224.763176117151815001-02513681015222943 FU50 FU0-3.28396228723762826.08964390824151281.45894095628794672.31315673357157442.1546869386277763-7.7593301236631049-8.96958913815083751.7993807839954035.8041390924723686001-03113681015222943 FU50 FU0-6.70446625203595661.5240951345269309-3.502344015089875-0.5673126431732527-1.62586011116198396.087195801657074415.49973640871765217.31663084569464718.29834889658008001-04813681015222943 FU50 FU0-11.667586529459882-14.181721366953809-9.1978685345636677-4.394488692808153-18.670351269288048-22.430724635824404-26.066410185794169-19.46058793671024-19.805501197617005001-06713681015222943 FU50 FU0-2.556697849055837-15.349225189902981-11.454260411495341-15.10248864544948311.896745779879765-5.94332990429889210.41762928087842965-2.5482977138357938-5.6334317522070876001-07313681015222943 FU50 FU07.52641733382411364.63714195923091673.6377846233778826-8.5967671913740702-11.417082794057364-6.640104123252982-9.6024350586344269-14.2283635169686421.5189286827857131

Days post-dosing


1.4201863080143344E-21.3605742643959806E-21.3014364363181728E-21.40536263610991E-21.5338876553403546E-22.1662010528917839E-21.6156654762101479E-21.7800765200529551E-21.8106020454888346E-21.5878788102320251E-21.4201863080143344E-21.3605742643959806E-21.3014364363181728E-21.40536263610991E-21.5338876553403546E-22.1662010528917839E-21.6156654762101479E-21.7800765200529551E-21.8106020454888346E-21.5878788102320251E-213681015222943 FU50 FU0.12902593576544760.130380281112132480.131120658124917830.130337819203013740.134379188297258510.119529178640989980.13692776172776830.134784047956284380.129162399688400850.12412649748003383

Days post-dosing


placebo03.05616172116967283.95622520632767753.41444426136847272.831315773442854212.7224337294368743.9832277527313665.94521999191763056.86257265277048936.593731228873279403.05616172116967283.95622520632767753.41444426136847272.831315773442854212.7224337294368743.9832277527313665.94521999191763056.86257265277048936.593731228873279413681015222943 FU50 FU0-1.6957180439390573-2.4290106719463034-1.3691246631411336-3.94847948897045388.4265120170106176-5.8613724112783432-3.64013113050866850.975435624579449214.1576099731943144

Days post-dosing


CL104_100mg

activeplacebo

subject code LGC33QIQ3

randomization nb101106102104105107109110103108

age group50-6465-7550-6450-6450-6465-7565-7565-7550-6465-75

subject IDVisit IDDay001-009001-011001-013001-022001-024001-026001-028001-065meansemCV%001-003001-025meansemCV%

serum-ARGS (pmol/ml)D1 pre-dose10.1000.1660.2260.1730.1950.2180.2700.1190.1830.0230.650.1090.1790.1440.0334.15

D3 pre-dose30.0930.1500.2230.1490.1650.1600.2300.1120.1600.0229.780.1020.1850.1440.0440.70

D6 pre-dose60.0710.1360.1850.1210.1440.1730.1720.0860.1360.0130.590.1060.1680.1370.0331.78

D8 pre-dose80.0640.1350.1740.1220.1500.1550.1630.0750.1300.0131.130.0980.1760.1370.0440.73

D10 pre-dose100.0420.1260.1730.1140.1450.1310.1510.0700.1190.0236.400.1070.1750.1410.0334.39

D15 pre-dose150.0680.1070.1520.0960.1390.1210.1350.0610.1100.0130.180.0350.1750.1050.0794.59

D22 pre-dose220.0500.1190.1640.1100.1310.1070.1450.0620.1110.0134.950.1080.1930.1500.0440.08

D29 pre-dose290.0550.1220.1540.1060.1350.1200.1630.0590.1140.0134.770.1020.1950.1490.0544.40

D43 FU43 FU0.1150.1760.2150.1860.2020.2050.3060.1320.1920.0230.280.0840.1760.1300.0549.79

D50 FU50 FU0.0980.1980.2280.1890.2290.2120.2680.1310.1940.0228.400.0820.1690.1260.0448.66

% reductionD1 pre-dose1000000000.000.00ERROR:#DIV/0!000.000.00ERROR:#DIV/0!

D3 pre-dose37.369.591.3713.8015.2726.6414.836.2311.892.7164.386.51-3.281.614.90429.17

D6 pre-dose629.3318.0117.9830.0426.4520.6736.4027.6225.812.2925.142.716.094.401.6954.40

D8 pre-dose835.8318.6222.9829.6322.9329.0139.7536.5629.412.6725.6810.841.466.154.69107.88

D10 pre-dose1057.9024.0623.2534.0125.6940.1544.1240.9436.274.2332.992.662.312.490.179.78

D15 pre-dose1531.8835.7932.7544.5428.8444.5350.0148.6539.622.9120.8068.222.1535.1933.03132.76

D22 pre-dose2249.7428.1927.2336.2232.9651.0146.3347.8139.943.4924.741.52-7.76-3.124.64-210.22

D29 pre-dose2944.5826.5831.8238.5530.7344.8139.7550.6438.432.9121.386.88-8.97-1.047.92-1072.85

D43 FU43 FU-14.86-5.954.71-7.70-3.696.04-13.62-11.04-5.762.77-135.8622.971.8012.3910.59120.88

D50 FU50 FU1.64-19.24-1.04-9.35-17.142.940.67-10.27-6.473.09-134.9924.765.8015.289.4887.72

1

3

6

8

10

15

22

29

43

50

CL101meansem

all placebo300mg600mg1050mgall placebo300mg600mg1050mg

CL101100000000

CL1013-0.889.0814.4212.102.962.460.961.15

CL1014-3.0317.9318.9022.183.392.861.981.41

CL1015-0.1516.9027.4528.811.913.512.971.13

CL1016-2.7719.0428.4132.892.603.932.541.45

CL1018-4.6330.4635.3340.672.652.531.960.82

CL10110-8.6339.0644.0646.414.793.082.701.69

CL101142.8552.1357.0160.344.481.652.211.53

CL101CL104

meansemmean 1972sem

all placebo300mg600mg1050mgall placebo300mg600mg1050mgplacebo100mg200mg300mgplacebo100mg200mg300mg

CL104D1 pre-dose1000000000.000.000.000.000.000.000.000.00

CL104D3 pre-dose3-0.889.0814.4212.102.962.460.961.15-1.7011.893.7112.793.062.712.402.28

4-3.0317.9318.9022.183.392.861.981.41

5-0.1516.9027.4528.811.913.512.971.13

CL104D6 pre-dose6-2.7719.0428.4132.892.603.932.541.45-2.4325.8121.4828.673.962.292.352.41

CL104D8 pre-dose8-4.6330.4635.3340.672.652.531.960.82-1.3729.4132.6739.923.412.672.382.48

CL104D10 pre-dose10-8.6339.0644.0646.414.793.082.701.69-3.9536.2738.3843.032.834.232.673.02

142.8552.1357.0160.344.481.652.211.53

CL104D15 pre-dose158.4339.6245.8653.4912.722.914.492.84

CL104D22 pre-dose22-5.8639.9445.7053.963.983.494.172.72

CL104D29 pre-dose29-3.6438.4344.9350.435.952.914.464.47

CL104D43 FU43 FU0.98-5.76-12.69-6.356.862.774.512.84

CL104D50 FUD50 FU4.16-6.47-14.38-11.596.593.095.633.91

1

3

4

5

6

8

10

14

15

22

29

43

50

001-00913681015222943 FU50 FU9.998268609660145E-29.2626352782684107E-27.0659262196799605E-26.4156118771503096E-24.2089940249094654E-26.81076450693648E-25.0250120333449153E-25.5409370097962998E-20.1148366813945119.8339291171802901E-2001-01113681015222943 FU50 FU0.16631491969390.150370394032817990.1363620114264780.135348533151179510.126293955302117010.1067907130843570.119427872875154990.122101117915841490.176215772521412990.1983061927862515001-01313681015222943 FU50 FU0.225895854582102980.22280341887592350.18528594328496450.173980627586924010.173382151975994490.151910550037538510.164386748082664510.154026138162091490.2152577305930960.22825016825543598001-02213681015222943 FU50 FU0.172861997524921480.149005273016965480.12094152246774950.12164039239301150.114067301447605499.5868136893265843E-20.11024885895732250.106220421877824490.1861768290466870.1890313221973455001-02413681015222943 FU50 FU0.19523269714617650.165412254309852010.143588961165263480.150469470821545490.1450742303257260.1389264952655980.130881768742504510.135231827353948010.202429231897176490.22869247434934398001-02613681015222943 FU50 FU0.218106192162258520.159997550958543010.173034328559808490.154830112622478010.130531702901106490.1209922964385810.1068539266217350.12037118365693650.204941524983542010.2116926884046155001-02813681015222943 FU50 FU0.269741218135481520.229728851470387990.171543300200844520.162518050996369510.150721393012872520.134856357908871020.144757011769837520.1625268733069250.3064674554733860.26792537009522249001-0650.1189874207848880.11157136522905258.612462647818625E-27.5488965583745099E-27.0269633143558455E-26.1103194539915695E-26.20954502149497E-25.8731919408265595E-20.132124565295773990.131208633107571001-0030.10941145794281150.10228659767458650.106450782224346019.754797421165684E-20.10650436978765853.4769939914737397E-20.10775052798615750.10188364119458018.4275432305949999E-28.2317705920089607E-2001-02513681015222943 FU50 FU0.17907705414343450.1849578770666010.16817189922473050.176464425657222010.174934721207234020.17521850424772650.19297223395015450.195139530140804510.17585477604263250.16868317283824752

Days post-dosing


001-00913681015222943 FU50 FU07.35760720292090329.32850180827317435.83277137651950357.90277107735621331.88056079673590749.74117790264365644.581034715923238-14.8565675496634531.6436795098810677001-01113681015222943 FU50 FU09.586948477278923518.00975421961533118.61912725551840724.06336392756641435.79005823355858228.19172621737115526.584386932593489-5.9530755543371328-19.235359732747327001-01313681015222943 FU50 FU01.368965230415739117.97727159370187222.98192992129925523.24686422566560432.75195318720385327.22896646918444231.815420673817674.7093046522199415-1.0422119864432204001-02213681015222943 FU50 FU013.80102327263492230.03579491188432429.63150135096950134.01250530431916344.54065192701214936.22145958285137438.551894922705195-7.7025787694290244-9.3538920664693279001-02413681015222943 FU50 FU015.27430767091080126.45240102493990322.92814010099725425.69163237185387128.84055934463701532.96114295623880330.733002549928443-3.6861319114040185-17.138408520840727001-02613681015222943 FU50 FU026.64236197406353320.66510040619073229.01159243232615440.15222511243587944.52596909831442751.008302165835944.8107444985389386.03589794870323712.9405418039996505001-02813681015222943 FU50 FU014.83361235693564636.40449116875999639.75038293378566644.12370713875457550.00528327074677346.33485650786556739.747112276591906-13.6153597851175190.67318152294656386001-06506.23263829648232127.61871304540075336.55718807434426140.94364540383158248.64734932747100547.81343287774153350.640228167946944-11.040784331846339-10.271012046539923001-00313681015222943 FU50 FU06.51198732033084582.706001523179608610.8429994026362522.657023505410663268.2209335580635641.51805851771224816.88028190993134122.97385128530132224.763176117151815001-0250-3.28396228723762826.08964390824151281.45894095628794672.31315673357157442.1546869386277763-7.7593301236631049-8.96958913815083751.7993807839954035.8041390924723686

Days post-dosing


GLPG1972 100mg02.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877802.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877813681015222943 FU50 FU011.88718306020534925.8115035223457629.41407918071999836.26708932022290839.62279814820996639.93763308496654938.432978092255723-5.7636619126092885-6.472935189526655404.8979748037842371.69182119253095284.69202922317415270.1719333859195444333.0331233097178944.63869432068767657.924935524041088410.5872352506529589.47951851233972504.8979748037842371.69182119253095284.69202922317415270.1719333859195444333.0331233097178944.63869432068767657.924935524041088410.5872352506529589.47951851233972513681015222943 FU50 FU01.61401251654660884.39782271571056076.15097017946209952.485090119491118835.18781024834567-3.1206358029754284-1.044653614109748212.38661603464836215.283657604812092

Days post-dosing


CL104 placebo03.05616172116967283.95622520632767753.41444426136847272.831315773442854212.7224337294368743.9832277527313665.94521999191763056.86257265277048936.593731228873279403.05616172116967283.95622520632767753.41444426136847272.831315773442854212.7224337294368743.9832277527313665.94521999191763056.86257265277048936.5937312288732794134568101415222943 FUD50 FU0-1.6957180439390573-2.4290106719463034-1.3691246631411336-3.94847948897045388.4265120170106176-5.8613724112783432-3.64013113050866850.975435624579449214.1576099731943144CL104 100mg02.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877802.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.089179918348778134568101415222943 FUD50 FU011.88718306020534925.8115035223457629.41407918071999836.26708932022290839.62279814820996639.93763308496654938.432978092255723-5.7636619126092885-6.4729351895266554CL104 200mg02.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781102.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781103.706339638082214421.4840962812108132.66887652175267938.37521256537915845.85912944049331945.7036166259120944.927042591134409-12.689923154782715-14.380494797641056CL104 300mg02.28481036718146812.40992799782371942.47819750042884123.01773941105111732.84339852029234042.71718102276922174.47066463189533622.84388318194113143.914163047530318202.28481036718146812.40992799782371942.47819750042884123.01773941105111732.84339852029234042.71718102276922174.47066463189533622.84388318194113143.9141630475303182012.7874555796888828.66601706390963939.91722411634599943.03256863984385253.48692930965581453.95655175943095150.429061712309981-6.3471478344633647-11.587607986329798CL101 placebo02.95702405196187533.38849492708269921.91406859758385782.60340527916125762.64802281715474974.78741667810343694.476648834054370402.95702405196187533.38849492708269921.91406859758385782.60340527916125762.64802281715474974.78741667810343694.4766488340543704134568101415222943 FUD50 FU0-0.87512776689758687-3.0311238316811426-0.15250606298673355-2.7697895933328454-4.6329101276054017-8.62875978938289022.8480061111511552CL101 300mg02.4618358988477922.86128028923161983.51169790356526423.92518858161868422.52520944712484323.08026894297649131.647351650103792802.4618358988477922.86128028923161983.51169790356526423.92518858161868422.52520944712484323.08026894297649131.6473516501037928134568101415222943 FUD50 FU09.08174753933993117.93052404259849616.90030675791852819.04103658244259430.4643033530524439.06080469471402252.128574791893186CL101 600mg00.96336382744730921.9813315799250592.97092950438773552.54430133652058641.9636863798354542.69780299899209512.206924530082176700.96336382744730921.9813315799250592.97092950438773552.54430133652058641.9636863798354542.69780299899209512.2069245300821767134568101415222943 FUD50 FU014.41675688797383318.90080454763387227.44773992484314528.41384724348311935.32673657725818144.0637296897171557.011551659167914CL101 1050mg01.14933924207250551.40800686934683041.13128617442282441.44765338922296240.819757083674555351.69356553215998541.52652781345838401.14933924207250551.40800686934683041.13128617442282441.44765338922296240.819757083674555351.69356553215998541.526527813458384134568101415222943 FUD50 FU012.10038872035543322.18129271302289528.81174945120352532.89381936138443140.66726172694136246.41234241444215860.339056514135592

Days post-dosing


CL104 placebo134568101415222943500-1.6957180439390573-2.4290106719463034-1.3691246631411336-3.94847948897045388.4265120170106176-5.8613724112783432-3.64013113050866850.975435624579449214.1576099731943144CL104 100mg02.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877802.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877813456810141522294350011.88718306020534925.8115035223457629.41407918071999836.26708932022290839.62279814820996639.93763308496654938.432978092255723-5.7636619126092885-6.4729351895266554CL104 200mg02.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781102.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781103.706339638082214421.4840962812108132.66887652175267938.37521256537915845.85912944049331945.7036166259120944.927042591134409-12.689923154782715-14.380494797641056CL104 300mg02.28481036718146812.40992799782371942.47819750042884123.01773941105111732.84339852029234042.71718102276922174.47066463189533622.84388318194113143.914163047530318202.28481036718146812.40992799782371942.47819750042884123.01773941105111732.84339852029234042.71718102276922174.47066463189533622.84388318194113143.9141630475303182012.7874555796888828.66601706390963939.91722411634599943.03256863984385253.48692930965581453.95655175943095150.429061712309981-6.3471478344633647-11.587607986329798CL101 placebo02.95702405196187533.38849492708269921.91406859758385782.60340527916125762.64802281715474974.78741667810343694.476648834054370402.95702405196187533.38849492708269921.91406859758385782.60340527916125762.64802281715474974.78741667810343694.4766488340543704134568101415222943500-0.87512776689758687-3.0311238316811426-0.15250606298673355-2.7697895933328454-4.6329101276054017-8.62875978938289022.8480061111511552CL101 300mg02.4618358988477922.86128028923161983.51169790356526423.92518858161868422.52520944712484323.08026894297649131.647351650103792802.4618358988477922.86128028923161983.51169790356526423.92518858161868422.52520944712484323.08026894297649131.64735165010379281345681014152229435009.08174753933993117.93052404259849616.90030675791852819.04103658244259430.4643033530524439.06080469471402252.128574791893186CL101 600mg00.96336382744730921.9813315799250592.97092950438773552.54430133652058641.9636863798354542.69780299899209512.206924530082176700.96336382744730921.9813315799250592.97092950438773552.54430133652058641.9636863798354542.69780299899209512.206924530082176713456810141522294350014.41675688797383318.90080454763387227.44773992484314528.41384724348311935.32673657725818144.0637296897171557.011551659167914CL101 1050mg01.14933924207250551.40800686934683041.13128617442282441.44765338922296240.819757083674555351.69356553215998541.52652781345838401.14933924207250551.40800686934683041.13128617442282441.44765338922296240.819757083674555351.69356553215998541.52652781345838413456810141522294350012.10038872035543322.18129271302289528.81174945120352532.89381936138443140.66726172694136246.41234241444215860.339056514135592

Days post-dosing


GLPG1972 100mg02.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877802.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.0891799183487781368101522294350011.88718306020534925.8115035223457629.41407918071999836.26708932022290839.62279814820996639.93763308496654938.432978092255723-5.7636619126092885-6.4729351895266554placebo04.8979748037842371.69182119253095284.69202922317415270.1719333859195444333.0331233097178944.63869432068767657.924935524041088410.5872352506529589.47951851233972504.8979748037842371.69182119253095284.69202922317415270.1719333859195444333.0331233097178944.63869432068767657.924935524041088410.5872352506529589.479518512339725136810152229435001.61401251654660884.39782271571056076.15097017946209952.485090119491118835.18781024834567-3.1206358029754284-1.044653614109748212.38661603464836215.283657604812092

Days post-dosing


CL104_200mg

randomization nb305304303308309301307310302306

age group50-6450-6450-6465-7565-7550-6465-7565-7550-6465-75

Visit IDDay001-053001-054001-055001-058001-059001-066001-070001-071meansemCV%001-067001-073meansemCV%

serum-ARGS (pmol/ml)D1 pre-dose10.2010.2320.1520.0970.1530.1990.1800.1730.1730.0123.500.1380.1570.1470.019.43

D3 pre-dose30.1860.2200.1630.0990.1350.2050.1650.1580.1660.0123.230.1410.1450.1430.002.13

D6 pre-dose60.1430.1660.1230.0830.1090.1740.1490.1330.1350.0122.020.1590.1500.1540.004.01

D8 pre-dose80.1280.1550.1090.0720.0920.1560.1160.1020.1160.0125.310.1530.1520.1520.000.84

D10 pre-dose100.1150.1360.0920.0600.0820.1520.1240.0970.1070.0128.180.1580.1710.1650.015.33

D15 pre-dose150.1020.1160.0820.0530.0620.1650.0820.0940.0950.0137.010.1210.1750.1480.0325.76

D22 pre-dose220.0900.1100.1020.0630.0600.1400.0820.0950.0930.0127.890.1460.1680.1570.019.89

D29 pre-dose290.0860.1190.1050.0610.0590.1340.0760.1140.0940.0129.450.1370.1720.1550.0216.15

D43 FU43 FU0.2140.2480.1820.1280.1570.1920.2320.1860.1930.0120.360.1410.1800.1600.0216.99

D50 FU50 FU0.2310.2400.1800.1330.1450.1990.2460.1900.1950.0121.650.1450.1550.1500.004.49

% reductionD1 pre-dose1000000000.000.00ERROR:#DIV/0!000.0000.00ERROR:#DIV/0!

D3 pre-dose37.065.31-7.28-1.5311.77-3.068.518.863.712.40183.08-2.567.532.4855.04286.93

D6 pre-dose628.4828.7219.3214.1328.3912.5217.2423.0921.482.3530.91-15.354.64-5.3569.99-263.86

D8 pre-dose835.9533.1728.3826.2839.5621.5935.3641.0632.672.3820.64-11.453.64-3.9087.55-273.06

D10 pre-dose1042.6241.5539.8238.2446.1523.5530.9044.1938.382.6719.70-15.10-8.60-11.8503.25-38.82

D15 pre-dose1549.2750.1946.2145.1259.3816.8454.3145.5545.864.4927.6711.90-11.420.24011.666873.73

D22 pre-dose2254.9152.7332.9435.0660.7129.5954.5345.1745.704.1725.80-5.94-6.64-6.2920.35-7.83

D29 pre-dose2956.8948.8430.9037.0361.3532.6157.6234.1644.934.4628.100.42-9.60-4.5925.01-154.28

D43 FU43 FU-6.80-6.76-19.91-31.76-2.503.19-29.17-7.81-12.694.51-100.42-2.55-14.23-8.3885.84-98.46

D50 FU50 FU-15.08-3.04-18.21-37.115.39-0.14-36.83-10.02-14.385.63-110.80-5.631.52-2.0573.58-245.84

1

3

6

8

10

15

22

29

43

50

CL101meansem

all placebo300mg600mg1050mgall placebo300mg600mg1050mg

CL101100000000

CL1013-0.889.0814.4212.102.962.460.961.15

CL1014-3.0317.9318.9022.183.392.861.981.41

CL1015-0.1516.9027.4528.811.913.512.971.13

CL1016-2.7719.0428.4132.892.603.932.541.45

CL1018-4.6330.4635.3340.672.652.531.960.82

CL10110-8.6339.0644.0646.414.793.082.701.69

CL101142.8552.1357.0160.344.481.652.211.53

CL101CL104

meansemmean 1972sem

all placebo300mg600mg1050mgall placebo300mg600mg1050mgplacebo100mg200mg300mgplacebo100mg200mg300mg

CL104D1 pre-dose1000000000.000.000.000.000.000.000.000.00

CL104D3 pre-dose3-0.889.0814.4212.102.962.460.961.15-1.7011.893.7112.793.062.712.402.28

4-3.0317.9318.9022.183.392.861.981.41

5-0.1516.9027.4528.811.913.512.971.13

CL104D6 pre-dose6-2.7719.0428.4132.892.603.932.541.45-2.4325.8121.4828.673.962.292.352.41

CL104D8 pre-dose8-4.6330.4635.3340.672.652.531.960.82-1.3729.4132.6739.923.412.672.382.48

CL104D10 pre-dose10-8.6339.0644.0646.414.793.082.701.69-3.9536.2738.3843.032.834.232.673.02

142.8552.1357.0160.344.481.652.211.53

CL104D15 pre-dose158.4339.6245.8653.4912.722.914.492.84

CL104D22 pre-dose22-5.8639.9445.7053.963.983.494.172.72

CL104D29 pre-dose29-3.6438.4344.9350.435.952.914.464.47

CL104D43 FU43 FU0.98-5.76-12.69-6.356.862.774.512.84

CL104D50 FUD50 FU4.16-6.47-14.38-11.596.593.095.633.91

1

3

4

5

6

8

10

14

15

22

29

43

50

001-05313681015222943 FU50 FU0.2005160291108960.18635207119426850.143417095956362510.128432482150461490.115065780975020.10172430651895369.0411590907557945E-28.6435106954689603E-20.214142352316250010.2307492901410455001-05413681015222943 FU50 FU0.23248962597007250.220139810529948490.165721973034378990.1553736512518970.13589145535499850.1158082579337890.10990842223202450.11894184563458650.248195275899691980.23956835530755699001-05513681015222943 FU50 FU0.152131232355798510.16319916843283150.122744141927307010.108954614796293019.1556783799191854E-28.1829376746775095E-20.102024740069461490.1051173400744560.182424934621972510.17983575484464501001-05813681015222943 FU50 FU9.7071756113414454E-29.8560320445371302E-28.3358340246201951E-27.1560110046842054E-25.9956178347294303E-25.3269608491211151E-26.3043208701367592E-26.1121398467589294E-20.127897139124735990.1330992075457465001-05913681015222943 FU50 FU0.152844961788649980.13486205239098650.109451920871169019.2373479681394505E-28.2311424941831801E-26.2079731302682399E-26.0049181664476751E-25.90789648566123E-20.156672015193654510.14460007421700899001-06613681015222943 FU50 FU0.198710316676895480.204785922802375010.1738349387097190.155812418908346520.151908426800124510.165237603481019510.13991180762767350.133902368618514010.192377825616619510.19899138605019701001-07013681015222943 FU50 FU0.179991339896433010.1646720882837740.148962249787276510.116351189161239990.124379882169018.2244948245754998E-28.1846666075520658E-27.6274427894526403E-20.232494388677139010.2462803385306985001-0710.172971245192057480.157637935212578020.1330385161695980.1019483410570899.65387679840643E-29.4188506464424643E-29.4837244001563292E-20.113884774057142010.186486112011378490.19030320181980701001-06713681015222943 FU50 FU0.137625883312351980.141144561310742990.1587503900615580.153389910380569480.15841081671279950.12125288184736750.145805443591310510.137051117325572010.141133000550446970.14537894352212549001-0730.157294258198367510.145455635884215510.150000300151990010.151572231860170990.170816479381079990.17525267388717350.167738760722637490.172398337192826490.179674657046150490.15490507059421749

Days post-dosing


001-05313681015222943 FU50 FU07.06375344626144428.47599436699135835.94901977665260542.61517072463941249.26874077348964754.91054191106311356.893667135764794-6.795627893577489-15.077727782764399001-05413681015222943 FU50 FU05.311985594451314828.71855148680407433.16964118136709841.54945417973562650.18777399181821952.72545096434857548.839934195645604-6.7554196726357247-3.0447506240109448001-05513681015222943 FU50 FU0-7.275255649771992219.31693444759727628.38116597815084739.81723385697522146.21132329001596232.93636126548290130.903511102433114-19.912875086244156-18.210936741807416001-05813681015222943 FU50 FU0-1.533468015369649614.12709156223601826.28122441378900538.23519760243742445.12347296058676735.05504461286284437.034827724577589-31.755254304152572-37.114247104213433001-05913681015222943 FU50 FU011.76545774700102228.39023308958245239.56393550666972946.14711274837446859.38385500169470560.71235782863998161.347129689295777-2.5038793298901685.3942815485418549001-06613681015222943 FU50 FU0-3.057519220483399612.51841292549698921.58815832310372723.5528233558558516.84498004716225229.59006358226926632.6142845234149093.1867953139909844-0.14144679451069919001-07013681015222943 FU50 FU08.51110482397302817.23921280157735235.35734039860560130.89674078731890554.30616367816433954.52744219659945257.623279020860281-29.169763840258241-36.828993368463273001-07108.864658378595947923.08633956940093441.06052659568280944.18796726769636545.54672578101460845.17167064603056334.159707337083233-7.8133604254943521-10.020137513900139001-06713681015222943 FU50 FU0-2.556697849055837-15.349225189902981-11.454260411495341-15.10248864544948311.896745779879765-5.94332990429889210.41762928087842965-2.5482977138357938-5.6334317522070876001-07307.52641733382411364.63714195923091673.6377846233778826-8.5967671913740702-11.417082794057364-6.640104123252982-9.6024350586344269-14.2283635169686421.5189286827857131

Days post-dosing


GLPG1972 200mg02.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781102.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781113681015222943 FU50 FU03.706339638082214421.4840962812108132.66887652175267938.37521256537915845.85912944049331945.7036166259120944.927042591134409-12.689923154782715-14.38049479764105605.04155759143997539.99318357456694887.54602251743661073.252860727037704811.6569142869685630.348387109477044935.01003216975642835.84003290156642323.576180217496399905.04155759143997539.99318357456694887.54602251743661073.252860727037704811.6569142869685630.348387109477044935.01003216975642835.84003290156642323.576180217496399913681015222943 FU50 FU02.4848597423841383-5.3560416153360322-3.908237894058729-11.8496279184117770.23983149291120043-6.2917170137759371-4.5924028888779986-8.3883306154022179-2.0572515347106872

Days post-dosing


CL104 placebo03.05616172116967283.95622520632767753.41444426136847272.831315773442854212.7224337294368743.9832277527313665.94521999191763056.86257265277048936.593731228873279403.05616172116967283.95622520632767753.41444426136847272.831315773442854212.7224337294368743.9832277527313665.94521999191763056.86257265277048936.5937312288732794134568101415222943 FUD50 FU0-1.6957180439390573-2.4290106719463034-1.3691246631411336-3.94847948897045388.4265120170106176-5.8613724112783432-3.64013113050866850.975435624579449214.1576099731943144CL104 100mg02.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877802.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.089179918348778134568101415222943 FUD50 FU011.88718306020534925.8115035223457629.41407918071999836.26708932022290839.62279814820996639.93763308496654938.432978092255723-5.7636619126092885-6.4729351895266554CL104 200mg02.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781102.39901221413676912.34791135439278922.38360639637435772.67252354096087524.48652127019099114.16944732215897324.46376385486775014.50557318744536065.63347945090781103.706339638082214421.4840962812108132.66887652175267938.37521256537915845.85912944049331945.7036166259120944.927042591134409-12.689923154782715-14.380494797641056CL104 300mg02.28481036718146812.40992799782371942.47819750042884123.01773941105111732.84339852029234042.71718102276922174.47066463189533622.84388318194113143.914163047530318202.28481036718146812.40992799782371942.47819750042884123.01773941105111732.84339852029234042.71718102276922174.47066463189533622.84388318194113143.9141630475303182012.7874555796888828.66601706390963939.91722411634599943.03256863984385253.48692930965581453.95655175943095150.429061712309981-6.3471478344633647-11.587607986329798CL101 placebo02.95702405196187533.38849492708269921.91406859758385782.60340527916125762.64802281715474974.78741667810343694.476648834054370402.95702405196187533.38849492708269921.91406859758385782.60340527916125762.64802281715474974.78741667810343694.4766488340543704134568101415222943 FUD50 FU0-0.87512776689758687-3.0311238316811426-0.15250606298673355-2.7697895933328454-4.6329101276054017-8.62875978938289022.8480061111511552CL101 300mg02.4618358988477922.86128028923161983.51169790356526423.92518858161868422.52520944712484323.08026894297649131.647351650103792802.4618358988477922.86128028923161983.51169790356526423.92518858161868422.52520944712484323.08026894297649131.6473516501037928134568101415222943 FUD50 FU09.08174753933993117.93052404259849616.90030675791852819.04103658244259430.4643033530524439.06080469471402252.128574791893186CL101 600mg00.96336382744730921.9813315799250592.97092950438773552.54430133652058641.9636863798354542.69780299899209512.206924530082176700.96336382744730921.9813315799250592.97092950438773552.54430133652058641.9636863798354542.69780299899209512.2069245300821767134568101415222943 FUD50 FU014.41675688797383318.90080454763387227.44773992484314528.41384724348311935.32673657725818144.0637296897171557.011551659167914CL101 1050mg01.14933924207250551.40800686934683041.13128617442282441.44765338922296240.819757083674555351.69356553215998541.52652781345838401.14933924207250551.40800686934683041.13128617442282441.44765338922296240.819757083674555351.69356553215998541.526527813458384134568101415222943 FUD50 FU012.10038872035543322.18129271302289528.81174945120352532.89381936138443140.66726172694136246.41234241444215860.339056514135592

Days post-dosing


CL104 placebo134568101415222943500-1.6957180439390573-2.4290106719463034-1.3691246631411336-3.94847948897045388.4265120170106176-5.8613724112783432-3.64013113050866850.975435624579449214.1576099731943144CL104 100mg02.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877802.7056391747178152.29451988816167772.67008224304091794.23036269825772052.91413492131089493.49382054003939622.90536250155883872.76845161092256213.08917991834877813456810141522294350011.88718306020534925.8115035223457629.41407918071999836.26708932022290839.62279814820996639.93763308496654938.432978092255723-5.7636619126092885-6.4729351895266554CL104 200mg02.3990122141367

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