Elisidepsin

Summary

Elisidepsin (IB-01212) is a synthetic cyclic depsipeptide derived from the marine organism Cephalodiscus gilchristi. It exerts anticancer activity by disrupting tumor cell membrane organization, leading to rapid cell death. It has been evaluated in Phase I/II clinical trials for advanced solid tumors including non-small cell lung cancer and head and neck cancer.

Mechanism of Action

Interacts with the lipid bilayer of cell membranes, particularly targeting membrane microdomains (lipid rafts), disrupting membrane integrity and causing rapid membrane permeabilization. This leads to loss of mitochondrial membrane potential, activation of apoptotic pathways, and cell death independent of classic receptor-mediated signaling.

Routes of Administration

Goals & Uses

• Treatment of non-small cell lung cancer (NSCLC)OncologyLow
• Anticancer activity in solid tumorsOncologyModerate
• Membrane-targeting cytotoxicityMechanistic/ResearchModerate
• Treatment of head and neck squamous cell carcinomaOncologyLow

Contraindications

• Severe hepatic impairmentOrganHighLiver function concerns
• Severe renal impairmentOrganModerateKidney function concerns
• Poor performance status (ECOG >2)Clinical StatusHigh

Adverse Effects

• Peripheral neuropathyNeurologicalUncommon
• Nausea and vomitingGastrointestinalCommon
• FatigueGeneralCommonLow energy or tiredness
• MyelosuppressionHematologicUncommon
• Elevated liver enzymesHepaticUncommonIncrease in AST/ALT or other hepatic markers
• Mucositis/stomatitisGastrointestinalUncommon

Drug Interactions

• CYP3A4 inhibitorsModerate
• Other cytotoxic chemotherapeuticsModerate

Population Constraints

• Pediatric patientsAgeRelative
• Breastfeeding womenReproductiveAbsolute
• Elderly patients (>75 years)AgeRelative
• Pregnant womenReproductiveAbsolute

Regulatory Status

• European UnionInvestigationalPharmaMar conducted trials in Europe; no EMA approval. Development has not progressed beyond Phase II.
• United StatesInvestigationalInvestigated under IND for advanced solid tumors; no FDA approval granted. Clinical development appears inactive.

Elisidepsin has not received regulatory approval in any jurisdiction. It was evaluated in Phase I and Phase II clinical trials sponsored by PharmaMar. Development appears to have stalled after limited efficacy signals in Phase II trials.

Evidence & Sources

No sources recorded yet.