Telcagepant

Summary

Telcagepant (CHEMBL236593) is a phase-3 clinical-stage small molecule; indicated across 1 condition including migraine disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 1 condition
• Clinical trials: 13
• Chemistry: 566.5 Da · C26H27F5N6O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL236593
Name	Telcagepant
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	11319053
Molecular formula	C26H27F5N6O3
Molecular weight	566.5
InChIKey	CGDZXLJGHVKVIE-DNVCBOLYSA-N

SMILES: C1C[C@H](C(=O)N(C[C@@H]1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5

IUPAC name: N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide

Also known as: Mk-0974, MK-0974, MK0974, Telcagepant, telcagepant, TELCAGEPANT, [3H]telcagepant

Parent form; salt/anhydrous children: CHEMBL2105656

Patent coverage: 100 distinct patent families (254 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 197 (78%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
	CGRP receptor	Antagonist	9.1

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Calcitonin-gene-related peptide receptor, CALCRL/RAMP1, Calcitonin gene-related peptide type 1 receptor, Calcitonin gene-related peptide 1, Calcitonin gene-related peptide 1.

Bioactivity

ChEMBL activities: 26 potent at pChembl ≥ 5 of 26 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CALCRL	9.11	Ki	0.77	nM	CHEMBL_ACT_13359893
CALCRL	9.11	Ki	0.77	nM	CHEMBL_ACT_13459564
CALCRL	9.11	Ki	0.77	nM	CHEMBL_ACT_15010701
CALCRL	9.11	Ki	0.77	nM	CHEMBL_ACT_1996352
RAMP1	9.11	Ki	0.77	nM	CHEMBL_ACT_20657841
RAMP1	9.11	Ki	0.77	nM	CHEMBL_ACT_29122342
CALCA	9.11	Ki	0.78	nM	CHEMBL_ACT_7844708
CALCRL	9.1	Ki	0.8	nM	CHEMBL_ACT_2712879
CALCRL	9.1	Ki	0.8	nM	CHEMBL_ACT_3010840
CALCRL	9.1	Ki	0.8	nM	CHEMBL_ACT_6180625
RAMP1	8.92	IC50	1.2	nM	CHEMBL_ACT_29122373
CALCRL	8.72	Kd	1.9	nM	CHEMBL_ACT_15010714
CALCRL	8.7	IC50	2	nM	CHEMBL_ACT_3010841
CALCRL	8.7	IC50	2	nM	CHEMBL_ACT_6180655
CALCRL	8.66	IC50	2.2	nM	CHEMBL_ACT_15010711
CALCRL	8.66	IC50	2.2	nM	CHEMBL_ACT_1996381
CALCA	8.66	IC50	2.2	nM	CHEMBL_ACT_7844728
CALCRL	8.62	IC50	2.4	nM	CHEMBL_ACT_2712880
CALCRL	8.43	Kd	3.71	nM	CHEMBL_ACT_15010752
CALCRL	7.96	IC50	11	nM	CHEMBL_ACT_15010712
CALCRL	7.96	IC50	11	nM	CHEMBL_ACT_1996405
CALCRL	7.96	IC50	11	nM	CHEMBL_ACT_2712881
RAMP1	7.96	IC50	11	nM	CHEMBL_ACT_29122383
CALCRL	7.96	IC50	11	nM	CHEMBL_ACT_3010842
CALCRL	7.96	IC50	11	nM	CHEMBL_ACT_6180685
P01256	5.92	Ki	1200	nM	CHEMBL_ACT_7844773

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

1 disease in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
migraine disorder	3	MONDO:0005277	MONDO:0005277

Clinical trials

Total trials: 13.

Phase distribution

Phase	Trials
PHASE1	5
PHASE3	4
PHASE2	3
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00432237	PHASE3	COMPLETED	Safety and Efficacy Study of MK0974 in the Acute Migraine (0974-016)
NCT00442936	PHASE3	COMPLETED	Study of Telcagepant (MK-0974) in Participants With Moderate to Severe Acute Migraine With or Without Aura (MK-0974-011)
NCT00483704	PHASE3	COMPLETED	Multiple Attacks Study to Compare the Efficacy and Safety of MK-0974 With Placebo for Acute Migraine (MK-0974-031)
NCT00662818	PHASE3	COMPLETED	Telcagepant (MK-0974) Treatment of Migraine in Participants With Stable Vascular Disease (MK-0974-034)
NCT01125774	PHASE2/PHASE3	COMPLETED	Telcagepant for Prevention of Menstrually Related Migraine in Female Participants With Episodic Migraine (MK-0974-065)
NCT00246337	PHASE2	COMPLETED	A Dose-Finding Study of MK0974 in Acute Migraine (MK0974-004)
NCT00758836	PHASE2	COMPLETED	A Study to Test the Safety and Effectiveness of MK-0974 (Telcagepant) Co-administered With Ibuprofen or Acetaminophen in Patients With Migraines With or Without Aura (MK-0974-046)
NCT00797667	PHASE2	TERMINATED	MK0974 (Telcagepant) for Migraine Prophylaxis in Patients With Episodic Migraine (0974-049)
NCT00701389	PHASE1	COMPLETED	Study to Evaluate the Safety, Tolerability, and Blood Pressure Effect of an Oral Dose of Sumatriptan Alone and in Combination With MK-0974 (Telcagepant) in Migraine Patients (0974-026)
NCT00966030	PHASE1	COMPLETED	Bioequivalence of the Tablet and Liquid-Filled Capsule Forms of MK0974 (0974-042)
NCT01209741	PHASE1	COMPLETED	Bioavailability of Variably Aged MK-0974 Tablets (MK-0974-038)(COMPLETED)
NCT01294709	PHASE1	COMPLETED	A Study to Assess the Safety, Tolerability, and Effects of MK-0974 (Telcagepant) on Exercise Tolerance in Patients With Stable Angina (MK-0974-014)
NCT01315847	PHASE1	COMPLETED	Positron Emission Tomography (PET) Study of Brain Calcitonin Gene-Related Peptide (CGRP) Receptor Occupancy After Telcagepant Administration (MK-0974-067)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).