Soblidotin

Auristatin/dolastatin Analogue (synthetic Peptide)Rx: ResearchCompound: Investigational

Also known as: Auristatin PE, Dolastatin 10 analogue, TZT-1027

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Soblidotin (TZT-1027) is a synthetic dolastatin 10 analogue and potent antitubulin antitumor peptide. It was evaluated in phase II clinical trials for various solid tumors including non-small cell lung cancer and soft tissue sarcoma. Development was largely discontinued after phase II results showed limited single-agent efficacy.

Mechanism of Action

Inhibits tubulin polymerization by binding to the vinca alkaloid site on tubulin, disrupting microtubule dynamics, arresting cells in G2/M phase, and inducing apoptosis in rapidly dividing tumor cells.

Routes of Administration

Intravenous

Goals & Uses

  • Non-small cell lung cancer treatmentOncologyModerate
  • Antitubulin antineoplastic activityOncologyModerate
  • ADC payload candidateOncologyLow
  • Soft tissue sarcoma treatmentOncologyModerate

Contraindications

  • Severe peripheral neuropathyNeurotoxicityHigh
  • Severe hepatic impairmentOrganHighLiver function concerns
  • PregnancyPopulationHighPotential fetal risk or insufficient safety data

Adverse Effects

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

Drug Interactions

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

Population Constraints

  • Pediatric patientsAgeRelative
  • Pregnant or lactating womenReproductiveAbsolute
  • Patients with pre-existing neuropathyNeurologicRelative

Regulatory Status

  • European UnionInvestigationalPhase II trials conducted but no marketing authorization sought or granted.
  • United StatesInvestigationalInvestigated under IND; never approved by the FDA. No active development known.
  • United KingdomUnknownNo specific UK regulatory filing identified.

Never received regulatory approval in any jurisdiction. Phase II clinical development was conducted in Japan (Teikoku Hormone/Dainippon Sumitomo Pharma) and internationally. No active IND or ongoing pivotal trials are known as of the knowledge cutoff.

Evidence & Sources

No sources recorded yet.

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