Olcegepant
Also known as: BIBN 4096 BS, BIBN4096BS, BIBR 1532, CGRP antagonist, Olcegepant
Source Olcegepant at Peptiology
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Summary
Olcegepant (BIBR 1532) is a synthetic cyclic peptide that selectively blocks the CGRP receptor. It was investigated for acute migraine treatment and administered intravenously, but it has not received regulatory approval.
Mechanism of Action
Competitive antagonism of the calcitonin gene‑related peptide (CGRP) receptor, blocking CGRP‑mediated vasodilation and nociceptive signaling
Routes of Administration
Goals & Uses
- Acute migraine treatmentNeurology / PainModerate
- Cluster headacheNeurology / PainLow
- Acute migraine reliefAnalgesicModerate
- CGRP pathway proof-of-conceptResearchHigh
Contraindications
- Severe hepatic impairmentOrganModerateLiver function concerns
- Severe cardiovascular diseaseCardiovascularModerate
- Hypersensitivity to olcegepant or excipientsAllergyHigh
- Known hypersensitivity to olcegepantAllergyHigh
Adverse Effects
- HypotensionCardiovascularUncommonLow blood pressure
- FlushingVascularCommonWarmth and redness of the skin
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- ParesthesiaNeurologicUncommonTingling or numbness sensation
- DizzinessNeurologicUncommonFeeling faint, lightheaded, or unsteady
- Infusion-site reactionsLocal / AdministrationUncommon
Drug Interactions
- Triptans (e.g., sumatriptan)Moderate
- TriptansLow
- CYP3A4 inhibitorsLow
Population Constraints
- PregnancyReproductive SafetyRelative
- Renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeRelative
- Pediatric patients (<18 y)AgeAbsolute
- Pregnant or lactating womenReproductiveRelative
Regulatory Status
- European UnionInvestigationalNot authorized by EMA
- United StatesInvestigationalNo FDA approval; clinical trial use only
- United KingdomInvestigationalNot licensed by MHRA
Development discontinued; not approved in US, EU, or UK. Investigational use only in clinical trials.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Olcegepant?
Olcegepant (BIBR 1532) is a synthetic cyclic peptide that selectively blocks the CGRP receptor. It was investigated for acute migraine treatment and administered intravenously, but it has not received regulatory approval.
What is Olcegepant used for?
Olcegepant is educationally associated with: Acute migraine treatment, Cluster headache, Acute migraine relief, CGRP pathway proof-of-concept. Educational only — not medical advice.
How is Olcegepant administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Olcegepant?
Reported adverse effects include: Hypotension, Flushing, Nausea, Paresthesia, Dizziness, Infusion-site reactions. This list is not exhaustive — consult a qualified clinician.
Who should avoid Olcegepant?
Recorded contraindications: Severe hepatic impairment, Severe cardiovascular disease, Hypersensitivity to olcegepant or excipients, Known hypersensitivity to olcegepant. Consult a qualified clinician before use.