MK-677

pharmacological · endocrine · musculoskeletal · Oral

MK-677. Orally-bioavailable non-peptide GHSR-1a agonist — same pharmacological target as ipamorelin / GHRP family but with much longer oral half-life (~6 h). Raises…

Orally-bioavailable non-peptide GHSR-1a agonist — same pharmacological target as ipamorelin / GHRP family but with much longer oral half-life (~6 h). Raises GH + IGF-1 24-h exposure. Phase II studies in hip fracture + fibromyalgia showed efficacy; Merck halted development due to CHF exacerbation signal.

PK: STRIPPED. THE CITATION IS AN ASSAY PAPER, NOT A PHARMACOKINETIC ONE — it develops an LC-MS/MS method for measuring this compound in human plasma at picogram levels and reports no disposition parameter at all, so the stored half-life is class 1. The indexed literature was swept for a replacement and contains none: the pharmacokinetic-sounding hits are medicinal-chemistry papers reporting ANIMAL bioavailability ("F(rat)=65%, F(dog)=44%"), a review, and equine doping-control mass spectrometry. Human trials of this compound were run and their parameters are not in any abstract I can reach, which is exactly the lgd-4033 situation: human data exist, and the record is still unauthorable under the verbatim rule.

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Sources: PMID:8768828