Cemadotin
Also known as: Dolastatin 15 analogue, LU103793, NSC D-669356
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Summary
Cemadotin (LU103793) is a synthetic water-soluble pentapeptide analogue of dolastatin 15, a natural antimitotic peptide. It was investigated as an anticancer agent in Phase I and Phase II clinical trials for various solid tumors and hematologic malignancies. Clinical development was largely halted due to dose-limiting cardiovascular toxicities and modest single-agent efficacy.
Mechanism of Action
Inhibits tubulin polymerization by binding to the vinca alkaloid site on beta-tubulin, preventing microtubule assembly and causing mitotic arrest at G2/M phase, leading to apoptosis in rapidly dividing cancer cells.
Routes of Administration
Goals & Uses
- Solid tumor treatmentOncologyModerate
- Hematologic malignancy treatmentOncologyLow
- Tubulin polymerization inhibitionPharmacological MechanismHigh
Contraindications
- Severe hepatic impairmentOrganHighLiver function concerns
- Cardiovascular disease / conduction disordersCardiacHigh
- Severe bone marrow suppressionHematologicModerate
Adverse Effects
- Peripheral neuropathyNeurologicalUncommon
- HypotensionCardiovascularCommonLow blood pressure
- Nausea and vomitingGastrointestinalCommon
- NeutropeniaHematologicCommonLow neutrophil count
- FatigueGeneralCommonLow energy or tiredness
- BradycardiaCardiovascularCommon
Drug Interactions
- CYP3A4 inhibitorsModerate
- Other cardiotoxic agentsHigh
- Other myelosuppressive agentsModerate
Population Constraints
- Elderly patients with cardiac comorbiditiesAge/CardiacRelative
- Pediatric patientsAgeRelative
- Pregnant or lactating womenReproductiveAbsolute
Regulatory Status
- European UnionInvestigationalEuropean clinical trials conducted (BASF/Knoll); never received EMA marketing authorization.
- United StatesInvestigationalInvestigated under IND but never approved by FDA; clinical development discontinued.
Never received regulatory approval in any jurisdiction. Development discontinued after Phase II trials showed cardiovascular toxicity (hypotension, bradycardia) and limited clinical benefit as a single agent. Served as a structural template for antibody-drug conjugate (ADC) warheads such as monomethyl auristatin E (MMAE).
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Cemadotin?
Cemadotin (LU103793) is a synthetic water-soluble pentapeptide analogue of dolastatin 15, a natural antimitotic peptide. It was investigated as an anticancer agent in Phase I and Phase II clinical trials for various solid tumors and hematologic malignancies. Clinical development was largely halted due to dose-limiting cardiovascular toxicities and modest single-agent efficacy.
What is Cemadotin used for?
Cemadotin is educationally associated with: Solid tumor treatment, Hematologic malignancy treatment, Tubulin polymerization inhibition. Educational only — not medical advice.
How is Cemadotin administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Cemadotin?
Reported adverse effects include: Peripheral neuropathy, Hypotension, Nausea and vomiting, Neutropenia, Fatigue, Bradycardia. This list is not exhaustive — consult a qualified clinician.
Who should avoid Cemadotin?
Recorded contraindications: Severe hepatic impairment, Cardiovascular disease / conduction disorders, Severe bone marrow suppression. Consult a qualified clinician before use.