Table 1.

Current CGRP antagonists/antibodies under investigation

Name	Type	Affinity* (Ki, nM)	Indication	Route of Administration	Efficacious Doses, mg	Current Stage in Clinical Trials	Reference Nos.
Olcegepant (BIBN4096BS)	Nonpeptide receptor antagonist	0.01	Acute migraine treatment	Intravenous	2.5	Phase II	100, 293, 311, 349
Telcegepant (MK-0974)	Nonpeptide receptor antagonist	0.8	Acute migraine treatment/prophylactic for episodic migraine	Oral	150, 300	Discontinued after phase III due to liver toxicity	76, 77, 180
MK-3207	Nonpeptide receptor antagonist	0.02	Acute migraine treatment	Oral	10, 100, 200	Discontinued after phase II due to liver toxicity	176, 349
BI 44370 TA	Nonpeptide receptor antagonist	Not reported	Acute migraine treatment	Oral	400	Phase II	92
BMS-927711	Nonpeptide receptor antagonist	0.027	Acute migraine treatment	Oral	75, 150, 300	Phase II	258, 266
BMS-742413	Nonpeptide receptor antagonist	0.023	Acute migraine treatment	Intranasal		Preclinical	68
MK-2918	Nonpeptide receptor antagonist	0.05	Acute migraine treatment	Oral		Preclinical	318
LY2951742	Humanized monoclonal antibody against CGRP		Prophylactic for episodic migraine/also in preclinical studies for osteoarthritic pain	Subcutaneous	150	Phase II results reported at 2014 AAN meeting; clinical trial NCT01625988	31, 95
ALD403	Humanized monoclonal antibody against CGRP		Prophylactic for episodic migraine	Intravenous	1,000	Phase I results reported at 2014 AAN meeting; clinical trial NCT01772524	145
AMG 334	Fully humanized monoclonal antibody against CGRP receptor		Prophylactic for episodic and chronic migraine/also in phase I for hot flashes associated with menopause	Subcutaneous	Not reported	Phase II ongoing; clinical trial NCT01952574
LBR-101	Fully humanized antibody against CGRP		Prophylactic for episodic and chronic migraine	Subcutaneous	Dose-ranging	Phase I -published Phase II ongoing	32

^*Affinity is given for human calcitonin gene-related peptide (CGRP) receptor.