Olcegepant | C38H47Br2N9O5 | CID 6918509 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities

However, previously investigated CGRP receptor antagonists, telcagepant and MK-3207, were discontinued during clinical development because of concerns about drug-induced liver injury. A subsequent effort to identify novel CGRP receptor antagonists less likely to cause hepatotoxicity led to the development of ubrogepant.

Adverse events happened in 20% vs 12% in those receiving placebo. 77 Olcegepant was discontinued because of difficulties in developing an oral formulation. Telcagepant (MK‐0974) was the first orally available CGRP‐RA. Telcagepant was generally well tolerated: 66/2660 (2.5%) on telcagepant and 36/1326 (2.7%) on placebo discontinued because of a clinical adverse event. The percentages of patients with clinical adverse events, laboratory adverse events, or discontinuation because of a laboratory adverse event were also similar between treatments. However, 13 patients receiving telcagepant, but none on placebo, developed aminotransferase elevations more than threefold above normal; therefore, the trial was prematurely terminated.

Clinical efficacy was not observed at doses under 300 mg, and as such, these doses were discontinued. Pain relief at 2 h was 68%, 48%, and MK0974 (Telcagepant) for Migraine Prophylaxis in Patients With Episodic Migraine (0974-049) - Full Text View. Olcegepant (BIBN-4096) est un antagoniste non peptidique puissant et sélectif du récepteur du peptide 1 lié au gène de la calcitonine (CGRP1) avec IC 50 de 0,03 nM et K i de 14,4 pM pour le CGRP humain.. Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC 50 of 0.03 nM and K i of 14.4 pM for human CGRP.

Similar elevations were seen in a short-term study of menstrual migraine [25, 26]. Although Merck’s drug telcagepant and a follow-on compound showed promise, the company discontinued development of both because of liver toxicity. Other companies appear to be developing similar drugs, however, said Dr. Rapoport.

29 Jul 2011 Discontinued - Phase-II/III for Migraine in USA (PO)

The percentages of patients with clinical adverse events, laboratory adverse events, or discontinuation because of a laboratory adverse event were also similar between treatments. However, 13 patients receiving telcagepant, but none on placebo, developed aminotransferase elevations more than threefold above normal; therefore, the trial was prematurely terminated.

Two compounds, telcagepant [46][47][48][49][50][51] [52] and MK-3207 [53] have been discontinued due to hepatotoxic side-effects, olcegepant has been discontinued as an oral formulation was too

Small-molecule calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated therapeutic efficacy for the treatment of migraine. However, previously investigated CGRP receptor antagonists, telcagepant and MK-3207, were discontinued durin Company Presenting New Safety and Efficacy Data for Telcagepant at the 14th International Headache Congress. PHILADELPHIA, PA, USA | September 10, 2009 | Merck & Co., Inc. today updated the status of the clinical development programs for telcagepant (MK-0974) and MK-3207, the Company's investigational oral calcitonin gene-related peptide (CGRP) receptor antagonists for the intermittent Merck discontinued a CGRP receptor antagonist, telcagepant, because of liver toxicity in 2011. Merck decided to exit the space entirely, selling its backup compound, ubrogepant, to Allergan for $250 million in cash, with an undisclosed milestone and royalty backend in 2015.

New monographs The Merck CGRP antagonist telcagepant does not contract or relax human “ Merck is discontinuing the clinical development program for telcagepant, the 6 Jul 2015 In July 2011, Merck announced that it had discontinued clinical development of an earlier investigational oral CGRP antagonist, Telcagepant 24 Apr 2018 Telcagepant, MK-3207, BI 44370 TA and rimegepant all significantly years, clinical development of the initial gepants had been discontinued.
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Merck Updates Status of Clinical Development Programs for Investigational CGRP Receptor Antagonist Treatments for Acute Migraine; MK-3207 Clinical Development Discontinued Company Presenting New MK0974 (Telcagepant) for Migraine Prophylaxis in Patients With Episodic Migraine (0974-049) - Study Results. Telcagepant was generally well tolerated: 66/2660 (2.5%) on telcagepant and 36/1326 (2.7%) on placebo discontinued because of a clinical adverse event. The percentages of patients with clinical adverse events, laboratory adverse events, or discontinuation because of a laboratory adverse event were also similar between treatments.

Pain relief at 2 h was 68%, 48%, and MK0974 (Telcagepant) for Migraine Prophylaxis in Patients With Episodic Migraine (0974-049) - Full Text View. Olcegepant (BIBN-4096) est un antagoniste non peptidique puissant et sélectif du récepteur du peptide 1 lié au gène de la calcitonine (CGRP1) avec IC 50 de 0,03 nM et K i de 14,4 pM pour le CGRP humain.. Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC 50 of 0.03 nM and K i of 14.4 pM for human CGRP.
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the class after the failure of Merck's investigational migraine drug, telcagepant. failures – in 2011 telcagepant was discontinued due to liver toxicity concerns.

Please note that a pediatric investigational plan is approved by PDCO for telcagepant. As a result of this action, pediatric development will be discontinued. Regardless, Merck discontinued the development of telcagepant and another compound MK-3207 in July 2011 due to liver toxicity. Currently, there are other novel CGRP receptor antagonists undergoing clinical trials, with little evidence of liver toxicity in the early phases, highlighting an exciting time for small molecule CGRP antagonist.

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However, previously investigated CGRP receptor antagonists, telcagepant and MK-3207, were discontinued during clinical development because of concerns about drug-induced liver injury. A subsequent effort to identify novel CGRP receptor antagonists less likely to cause hepatotoxicity led to the development of ubrogepant.

16 The efficacy and safety of atogepant in migraine prevention was demonstrated in a phase IIb/III clinical trial conducted subsequent to this trial in which treatment with atogepant, compared with placebo MK0974 (Telcagepant) for Migraine Prophylaxis in Patients With Episodic Migraine (0974-049) - Full Text View. Telcagepant was generally well tolerated: 66/2660 (2.5%) on telcagepant and 36/1326 (2.7%) on placebo discontinued because of a clinical adverse event. The percentages of patients with clinical adverse events, laboratory adverse events, or discontinuation because of a laboratory adverse event were also similar between treatments. Fewer triptan related and drug‐related AEs were reported for telcagepant compared to rizatriptan (difference: −6.2% P < .001 and −15.6%, respectively). More patients discontinued telcagepant 300 mg (38.2%) than rizatriptan 10 mg (30.9%) Phase II‐III In addition, although telcagepant and BI 44370 were associated with moderate efficacy and low toxicity in acute intermittent treatment, research regarding these compounds has been discontinued due to hepatotoxicity concerns during long-term prophylactic use (Connor et al., 2011; Diener et al., 2011). Pooled together, all doses had a response rate of 60%.