Tasidotin
Also known as: Dolastatin 15 analogue, ILX651, LU 103793 analogue
Source Tasidotin at Peptiology
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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.
Frequently Asked Questions
What is Tasidotin?
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.
What is Tasidotin used for?
Tasidotin is educationally associated with: Solid tumor treatment, Antimitotic cancer therapy, Hematologic malignancy treatment. Educational only — not medical advice.
How is Tasidotin administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Tasidotin?
Reported adverse effects include: Peripheral neuropathy, Alopecia, Constipation, Nausea and vomiting, Neutropenia, Fatigue. This list is not exhaustive — consult a qualified clinician.
Who should avoid Tasidotin?
Recorded contraindications: Severe hepatic impairment, Pregnancy, Severe pre-existing neuropathy. Consult a qualified clinician before use.