A 4th Generation Antipsychotic and Sexual Entactogenic Drug

(Marketing Brief)

A New Way in Emotional Disorders and Sexual Therapy

Authors: Simon, Lehel &

Répási, József

Main scientific source and expert:

Dr. Molnár, László

The Starting Point of the Medicine:

The Expected Hit• V1/V3 antagonist Manning- peptide:

• X=D-Tyr-Phe-Val-Asn-Arg-Pro-Arg-Arg-NH2

http://endo.endojournals.org/content/138/10/4109.full.pdf

It is a free source molecule, what we would like to test pharmacodinamically. Our aim to develope a PET tracer with Fluor18 dervative of this peptide. In this way we could test the receptor affinity, so it is possible a research with other analogues molecules of AVP

O

X

The API• Our molecule is relatively simple peptide• It could be produced in standard peptide labs

or manufacturing facilities• The molecule is derived from a free source

(see attached file), YOU CAN OPEN IT IN OUTLOOK

http://books.google.hu/books?id=3VH5kb1DEGUC&pg=PA153&lpg=PA153&dq=D-Tyr-Phe-Val-Asn-Arg-Pro-Arg-Arg-NH2&source=bl&ots=-2vrDltgyx&sig=JV_0C1Sz_4yyofv_Yoy5QtRHhy8&hl=hu&ei=T6QdTayWIcaD5Abggd2GAg&sa=X&oi=book_result&ct=result&sqi=2&redir_esc=y#v=onepage&q=D-Tyr-Phe-Val-Asn-Arg-Pro-Arg-Arg-

NH2&f=false

but the therapeutic use could be patented

Is it a Hormone?

• It is similar to hormones, but it doesn't have hormonal effects like steroids, because it does not have any effects on V2 renal receptors. Other researchers determined the receptor affinities - see attached links

http://joe.endocrinology-journals.org/content/141/3/383.abstract http://www.ncbi.nlm.nih.gov/pubmed/8071638

• This is analogue to a hormone AVP and expected to act mainly in the brain

Potential Applications of the Medicine

It is a fairly stable peptide and could be used in intravenous injection or as a transdermal patch

Primary suggested usage: therapy of negativism (autisms and adults’ negativistic disorders)

Other major application: sextherapy

These are valid in all mammals, see

http://www.ncbi.nlm.nih.gov/pubmed/9951561 http://www.ncbi.nlm.nih.gov/pubmed/22141469 http://www.ncbi.nlm.nih.gov/pubmed/18655893

Cost and Value

• The market value of this drug is huge, because only micrograms are needed from the drug, and it can be produced from very cheap ingredients using standard peptide synthesis procedures. It verified our thesis, that far less receptors are in the brain, than in the kidney; and the V2 (renal) vasopressin-agonist desmopressin’s dose is 0, 1-0,6 mg

Cost and Value

• It is very economical: the expected manufacturing cost in industrial scale would be tens of thousand USD/kg

• In comparison rats received from the concurrent complicated polycyclic

• The expected dose is 10-100 μg/kg

• SSR vaptans are used in 10-30 mg/kg dose

Experimental Introduction

• We would like the experimental introduction of this molecule from other direct researches:

• http://www.ncbi.nlm.nih.gov/pubmed/8071638http://joe.endocrinology-journals.org/cgi/content/abstract/141/3/383

• The estimated cost of proof of concept work expected to be in the range of 1 - 1,5 million dollars plus the experimental cost - see attached file