Telcagepant (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway. Before the advent of motorized transportation, they also provided accomm ...

; development code MK-0974) is a

calcitonin gene-related peptide receptor antagonist Calcitonin gene-related peptide (CGRP) receptor antagonists, commonly known as gepants, are a class of drugs that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR). Several monoclonal antibodies that bind to the CGRP rece ...

which was an investigational drug for the acute treatment and prevention of

migraine Migraine (, ) is a complex neurological disorder characterized by episodes of moderate-to-severe headache, most often unilateral and generally associated with nausea, and light and sound sensitivity. Other characterizing symptoms may includ ...

, developed by Merck & Co. In the acute treatment of migraine, it was found to have equal efficacy to

rizatriptan Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches. It is taken by mouth. It can also be applied on the tongue. It is a serotonin (5-HT) 1B/1D receptor agonist (triptan). ...

and

zolmitriptan Zolmitriptan, sold under the brand name Zomig among others, is a serotonergic drug, serotonergic medication which is used in the acute treatment of migraine attacks with or without aura (symptom), aura and cluster headaches. It is taken oral adm ...

. A

Phase IIa The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phases ...

clinical trial studying telcagepant for the

prophylaxis Preventive healthcare, or prophylaxis, is the application of healthcare measures to prevent diseases.Hugh R. Leavell and E. Gurney Clark as "the science and art of preventing disease, prolonging life, and promoting physical and mental health a ...

of episodic migraine was stopped on March 26, 2009, after the "identification of two patients with significant elevations in serum transaminases". A memo to study locations stated that telcagepant had preliminarily been reported to increase the hepatic liver enzyme

alanine transaminase Alanine aminotransferase (ALT or ALAT), formerly alanine transaminase (ALT), and even earlier referred to as serum glutamate-pyruvate transaminase (GPT) or serum glutamic-pyruvic transaminase (SGPT), is a transaminase enzyme () that was first c ...

(ALT) levels in "11 out of 660 randomized (double-blinded) study participants." All study participants were told to stop taking the medication. In July 2011, Merck announced that it had discontinued development of telcagepant.

References

{{Antimigraine preparations Abandoned drugs Antimigraine drugs Azepanes Imidazopyridines Lactams Fluoroarenes Piperidines Calcitonin gene-related peptide receptor antagonists Ureas Trifluoroethyl compounds

See also

References