Delving into the Latest Updates on L-739943 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

GHRHR

Mechanism

GHRHR agonists(GHRH receptor agonists)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Merck & Co., Inc.

Active Organization-

Inactive Organization-

Drug Highest Phase-

First Approval Date-

Regulation-

Structure

Molecular FormulaC30H36ClN5O3

InChIKeyCQCCAABVCYEOTD-VQIWEWKSSA-N

CAS Registry195248-02-3

Author: Jacks, Thomas M. ; Cunningham, Paul K. ; Chan, Wanda W.-S. ; Chen, Zhesheng ; Smith, Roy G. ; Leung, Kwan ; Cheng, Kang ; Fisher, Michael H. ; Feeney, William P. ; Hickey, Gerard J. ; Schoen, William R. ; Bochis, Richard ; Kotliar, Andrew ; Butler, Bridget ; Frontier, Alison J. ; Wyvratt, Matthew J. ; Chiu, S.-H. Lee ; DeVita, Robert J. ; Schleim, Klaus D.

The identification of L-739,943 (8b), a potent, orally bioavailable benzolactam growth hormone secretagogue, is obtained from zwitterionic L-692,429 through modification of its amino acid side chain and replacement of the acidic 2'-tetrazole with the neutral and potency enhancing 2'-(N-methylaminocarbonylamino)methyl substituent. L-739,943 is orally active for the release of growth hormone in beagle dogs at doses as low as 0.5 mg/kg. Oral bioavailability in dogs of 8b is 24% at a dose of 2 mg/kg with a mean drug Cmax of 145 +/- 46 ng/mL. L-739,943 represents a significant breakthrough in terms of both potency and oral bioavailability as compared to the prototype benzolactam L-692,429.

100 Deals associated with L-739943

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