MK-0773

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C27H34FN5O2
Molecular Weight	479.5896
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1[C@@H]2CC[C@H]3[C@@H]4CC[C@H](C(=O)NCC5=NC6=NC=CC=C6N5)[C@@]4(C)CC[C@@H]3[C@@]2(C)C=C(F)C1=O

InChI

InChIKey=GBEUKTWTUSPHEE-JWJWXJQQSA-N

InChI=1S/C27H34FN5O2/c1-26-11-10-17-15(6-9-21-27(17,2)13-19(28)25(35)33(21)3)16(26)7-8-18(26)24(34)30-14-22-31-20-5-4-12-29-23(20)32-22/h4-5,12-13,15-18,21H,6-11,14H2,1-3H3,(H,30,34)(H,29,31,32)/t15-,16-,17-,18+,21+,26-,27+/m0/s1

HIDE SMILES / InChI

Description

MK-0773 is an orally active selective androgen receptor modulator. The safety and efficacy of MK-0773 was evaluated in sarcopenic elderly women. The MK-0773- induced improvements in lean body mass were not accompanied by statistically significant improvements in physical function. Higher dose of MK-0773 or longer duration of therapy might have resulted in improvements in physical function, but liver transaminase elevations likely preclude further development of MK-0773. Drug-candidate had been in phase I clinical trials for the treatment of osteoporosis.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Androgen Receptor 153	Partial Agonist 249	Sarcopenia	6.6 nM [IC50]
HERG 82	Binding Agent 942		49.5 µM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Sarcopenia 3	Primary	Androgen Receptor	Phase II 1085
Osteoporosis 124	Primary	Androgen Receptor	Phase I 395

PubMed

Title	Date	PubMed
Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology.	2010 May 28	20356837
A phase IIA randomized, placebo-controlled clinical trial to study the efficacy and safety of the selective androgen receptor modulator (SARM), MK-0773 in female participants with sarcopenia.	2013	23732550
Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer.	2013 Dec	24189892
Identification of selected in vitro generated phase-I metabolites of the steroidal selective androgen receptor modulator MK-0773 for doping control purposes.	2016	27419898
Detection of SARMs in doping control analysis.	2018 Mar 15	28137616

Patents

Sample Use Guides

In Vivo Use Guide

50 mg twice daily, 6 month treatment period

Route of Administration: Oral

In Vitro Use Guide

The affinity of MK-0773 for AR across species was evaluated using COS cells transfected with AR, and IC50 values were very similar in four species (rat, 0.50 nM; dog, 0.55 nM; rhesus, 0.45 nM; human, 0.65 nM).

Name

Type

Language

MK-0773

Common Name

English

PF-05314882

Code

English

N-(3H-IMIDAZO(4,5-B)PYRIDIN-2-YLMETHYL)-2-FLUORO-4-METHYL-3-OXO-4-AZA-5.ALPHA.-ANDROST-1-ENE-17.BETA.-CARBOXAMIDE

Systematic Name

English

Code System Code Type Description

ChEMBL

CHEMBL3545333

Created by admin on Tue Oct 22 15:40:50 UTC 2019 , Edited by admin on Tue Oct 22 15:40:50 UTC 2019

PRIMARY

PUBCHEM

11950726

Created by admin on Tue Oct 22 15:40:50 UTC 2019 , Edited by admin on Tue Oct 22 15:40:50 UTC 2019

PRIMARY

CAS

606101-58-0

Created by admin on Tue Oct 22 15:40:50 UTC 2019 , Edited by admin on Tue Oct 22 15:40:50 UTC 2019

PRIMARY

WIKIPEDIA

MK-0773

Created by admin on Tue Oct 22 15:40:50 UTC 2019 , Edited by admin on Tue Oct 22 15:40:50 UTC 2019

PRIMARY

ACTIVE MOIETY


					5730VNW22X

MK-0773