Tasidotin

Summary

Tasidotin (ILX651) is a synthetic analogue of dolastatin 15, a natural peptide derived from the sea hare Dolabella auricularia. It is an antimitotic agent that inhibits tubulin polymerization. Tasidotin was evaluated in multiple Phase I and Phase II clinical trials for various solid tumors and hematologic malignancies. Clinical development was ultimately limited by modest single-agent activity and tolerability concerns.

Mechanism of Action

Inhibits tubulin polymerization by binding to the vinca alkaloid domain of tubulin, disrupting microtubule dynamics and causing mitotic arrest leading to apoptosis.

Routes of Administration

Goals & Uses

• Solid tumor treatmentOncologyModerate
• Antimitotic cancer therapyOncologyModerate
• Hematologic malignancy treatmentOncologyLow

Contraindications

• Severe hepatic impairmentOrganHighLiver function concerns
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Severe pre-existing neuropathyNeurologicalModerate

Adverse Effects

• Peripheral neuropathyNeurologicalUncommon
• AlopeciaDermatologicUncommonHair loss
• ConstipationGastrointestinalUncommonReduced bowel frequency or difficulty passing stool
• Nausea and vomitingGastrointestinalCommon
• NeutropeniaHematologicCommonLow neutrophil count
• FatigueGeneralCommonLow energy or tiredness

Drug Interactions

• CYP3A4 inhibitors (e.g., ketoconazole)Moderate
• Other myelosuppressive agentsHigh

Population Constraints

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

Regulatory Status

• European UnionInvestigationalNo EMA approval; limited European clinical trial participation.
• United StatesInvestigationalStudied under IND; never received FDA approval. Development discontinued after Phase II.

Tasidotin has not received regulatory approval in any jurisdiction. It was studied under IND status in the United States as an investigational anticancer agent. Development appears to have stalled after Phase II trials showed insufficient efficacy.

Evidence & Sources

No sources recorded yet.