Dolastatin 10
Also known as: Dol-10, Dola-10, Dolastatin-10, NSC-376128
Source Dolastatin 10 at Peptiology
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Summary
Dolastatin 10 is a linear non‑ribosomal peptide isolated from the sea hare Dolabella auricularia. It exhibits potent antimitotic activity and has been evaluated in early‑phase oncology trials, but development was halted because of dose‑limiting toxicities.
Mechanism of Action
Binds to tubulin at the Vinca site, inhibiting microtubule polymerization and causing G2/M cell‑cycle arrest.
Routes of Administration
Goals & Uses
- Anticancer activityOncologyModerate
- Cancer chemotherapyOncologyModerate
- Tubulin inhibition researchBasic ResearchHigh
- ADC payload scaffoldDrug DevelopmentHigh
Contraindications
- Severe hepatic impairmentOrganModerateLiver function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Severe bone marrow suppressionHematologicHigh
Adverse Effects
- Peripheral neuropathyNeurologicalCommon
- Myelosuppression / neutropeniaHematologicCommon
- AlopeciaDermatologicCommonHair loss
- ConstipationGastrointestinalUncommonReduced bowel frequency or difficulty passing stool
- Nausea and vomitingGastrointestinalCommon
- NeutropeniaHematologicCommonLow neutrophil count
- FatigueGeneralCommonLow energy or tiredness
Drug Interactions
- Vinca alkaloidsModerate
- CYP3A4 inhibitors (e.g., ketoconazole)Moderate
- Other myelosuppressive agentsHigh
Population Constraints
- PregnancyReproductive SafetyAbsolute
- Pediatric patientsAgeRelative
- Severely immunocompromised patientsImmunologicalRelative
- Pregnant womenReproductiveAbsolute
- Patients with pre-existing neuropathyNeurologicRelative
Regulatory Status
- European UnionInvestigationalSame as US.
- United StatesInvestigationalPhase I/II trials discontinued; not approved.
- United KingdomUnapprovedNo MHRA approval; research compound only
No regulatory approval; clinical development discontinued due to severe myelosuppression and neurotoxicity.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Dolastatin 10?
Dolastatin 10 is a linear non‑ribosomal peptide isolated from the sea hare Dolabella auricularia. It exhibits potent antimitotic activity and has been evaluated in early‑phase oncology trials, but development was halted because of dose‑limiting toxicities.
What is Dolastatin 10 used for?
Dolastatin 10 is educationally associated with: Anticancer activity, Cancer chemotherapy, Tubulin inhibition research, ADC payload scaffold. Educational only — not medical advice.
How is Dolastatin 10 administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Dolastatin 10?
Reported adverse effects include: Peripheral neuropathy, Myelosuppression / neutropenia, Alopecia, Constipation, Nausea and vomiting, Neutropenia, Fatigue. This list is not exhaustive — consult a qualified clinician.
Who should avoid Dolastatin 10?
Recorded contraindications: Severe hepatic impairment, Pregnancy, Severe bone marrow suppression. Consult a qualified clinician before use.