Telcagepant
Encyclopedia
Telcagepant was an investigational drug for the acute treatment and prevention of migraine
, developed by Merck & Co.
In the acute treatment of migraine, it was found to have equal potency to rizatriptan
and zolmitriptan
in two Phase III clinical trial
s. The company has now terminated development of the drug.
(CGRP) is a strong vasodilator primarily found in nervous tissue. Since vasodilation in the brain is thought to be involved in the development of migraine and CGRP levels are increased during migraine attacks, this peptide may be an important target for potential new antimigraine drugs.
Telcagepant acts as a calcitonin gene-related peptide receptor (CRLR) antagonist and blocks this peptide
. It is believed to constrict dilated blood vessels within the brain.
A memo to study locations stated that telcagepant had preliminarily been reported to increase the hepatic liver enzyme alanine transaminase
(AST) levels in "11 out of 660 randomized (double-blinded) study participants." All study participants were told to stop taking the medication.
On July 29, 2011, it was reported that Merck & Co. were discontinuing the clinical development program for telcagepant. According to Merck, "[t]he decision is based on an assessment of data across the clinical program, including findings from a recently completed six-month Phase III study".
Migraine
Migraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...
, developed by Merck & Co.
Merck & Co.
Merck & Co., Inc. , also known as Merck Sharp & Dohme or MSD outside the United States and Canada, is one of the largest pharmaceutical companies in the world. The Merck headquarters is located in Whitehouse Station, New Jersey, an unincorporated area in Readington Township...
In the acute treatment of migraine, it was found to have equal potency to rizatriptan
Rizatriptan
Rizatriptan is a 5-HT1 agonist triptan drug developed by Merck & Co. for the treatment of migraine headaches. It is available in strengths of 5 and 10 mg as tablets and orally disintegrating tablets ....
and zolmitriptan
Zolmitriptan
Zolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is a triptan, used in the acute treatment of migraine attacks with or without aura and cluster headaches....
in two Phase III clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
s. The company has now terminated development of the drug.
Mechanism of action
The calcitonin gene-related peptideCalcitonin gene-related peptide
Calcitonin gene related peptide is a member of the calcitonin family of peptides, which in humans exists in two forms, α-CGRP and β-CGRP. α-CGRP is a 37-amino acid peptide and is formed from the alternative splicing of the calcitonin/CGRP gene located on chromosome 11...
(CGRP) is a strong vasodilator primarily found in nervous tissue. Since vasodilation in the brain is thought to be involved in the development of migraine and CGRP levels are increased during migraine attacks, this peptide may be an important target for potential new antimigraine drugs.
Telcagepant acts as a calcitonin gene-related peptide receptor (CRLR) antagonist and blocks this peptide
Peptide
Peptides are short polymers of amino acid monomers linked by peptide bonds. They are distinguished from proteins on the basis of size, typically containing less than 50 monomer units. The shortest peptides are dipeptides, consisting of two amino acids joined by a single peptide bond...
. It is believed to constrict dilated blood vessels within the brain.
Termination of a clinical trial
A Phase IIa clinical trial studying telcagepant for the prophylaxis 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 transaminase
Alanine transaminase or ALT is a transaminase enzyme . It is also called serum glutamic pyruvic transaminase or alanine aminotransferase ....
(AST) levels in "11 out of 660 randomized (double-blinded) study participants." All study participants were told to stop taking the medication.
On July 29, 2011, it was reported that Merck & Co. were discontinuing the clinical development program for telcagepant. According to Merck, "[t]he decision is based on an assessment of data across the clinical program, including findings from a recently completed six-month Phase III study".