Olcegepant

Summary

Olcegepant (BIBN4096BS) was the first CGRP receptor antagonist demonstrated to be effective in acute migraine treatment in clinical trials. It is a peptidomimetic administered intravenously and proved proof-of-concept for the CGRP pathway in migraine. It was not developed further commercially due to its IV route, but it paved the way for oral gepants such as ubrogepant and rimegepant.

Mechanism of Action

Competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor; blocks CGRP-mediated vasodilation and neurogenic inflammation implicated in migraine pathophysiology without vasoconstriction

Routes of Administration

Goals & Uses

• Acute migraine treatmentNeurology / PainModerate
• Cluster headacheNeurology / PainLow
• CGRP pathway proof-of-conceptResearchHigh

Contraindications

• Severe hepatic impairmentOrganModerateLiver function concerns
• Hypersensitivity to olcegepant or excipientsAllergyHigh

Adverse Effects

• NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
• ParesthesiaNeurologicUncommonTingling or numbness sensation
• DizzinessNeurologicUncommonFeeling faint, lightheaded, or unsteady
• Infusion-site reactionsLocal / AdministrationUncommon

Drug Interactions

• TriptansLow
• CYP3A4 inhibitorsLow

Population Constraints

• PregnancyReproductive SafetyRelative
• Renal impairmentOrgan ImpairmentRelative
• Pediatric patientsAgeRelative

Regulatory Status

• European UnionUnapprovedNo EMA approval; Boehringer Ingelheim discontinued development
• United StatesUnapprovedNever submitted for or received FDA approval; development discontinued after Phase II
• United KingdomUnapprovedNo MHRA approval; research compound only

Never received regulatory approval in any jurisdiction. Development was discontinued after Phase II trials; served primarily as a proof-of-concept compound.

Evidence & Sources

No sources recorded yet.