Canfosfamide
Also known as: canfosfamide hydrochloride, Telcyta, TLK286
Source Canfosfamide at Peptiology
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Summary
Canfosfamide (TLK286) is an investigational glutathione analog prodrug designed for selective activation by GST Pi-overexpressing tumor cells. It was evaluated in clinical trials for ovarian cancer, non-small cell lung cancer, and other solid tumors. Despite encouraging early results, Phase III trials did not demonstrate sufficient efficacy to support regulatory approval, and development was largely discontinued.
Mechanism of Action
Canfosfamide is a glutathione analog conjugated to a phosphorodiamide mustard alkylating agent. It is selectively activated by glutathione S-transferase Pi (GST Pi), which is overexpressed in many tumor cells, releasing an alkylating moiety that cross-links DNA and induces apoptosis in cancer cells.
Routes of Administration
Goals & Uses
- Colorectal cancer treatmentOncologyLow
- Ovarian cancer treatmentOncologyModerate
- Tumor-selective cytotoxicity via GST Pi overexpressionMechanismModerate
- Non-small cell lung cancer treatmentOncologyLow
Contraindications
- Hypersensitivity to canfosfamide or its componentsAllergyHigh
- Severe bone marrow suppressionHematologicHigh
Adverse Effects
- ThrombocytopeniaHematologicCommonLow platelet count
- AnemiaHematologicCommonLow red blood cell count or hemoglobin
- HypotensionCardiovascularUncommonLow blood pressure
- Nausea and vomitingGastrointestinalCommon
- NeutropeniaHematologicCommonLow neutrophil count
- FatigueGeneralCommonLow energy or tiredness
Drug Interactions
- Platinum-based chemotherapy (e.g., carboplatin)Moderate
- Other myelosuppressive agentsHigh
Population Constraints
- PregnancyReproductive SafetyAbsolute
- Severe renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeRelative
- Severe hepatic impairmentOrgan ImpairmentRelative
Regulatory Status
- European UnionInvestigationalEvaluated in European clinical trials; no marketing authorization granted
- United StatesInvestigationalReceived Fast Track designation from FDA for ovarian cancer; Phase III trials failed; never approved
- United KingdomInvestigationalNo approval; development discontinued following negative Phase III results
Never received FDA, EMA, or other major regulatory approval. Phase III clinical trials (e.g., ASSIST-1, ASSIST-2 in ovarian cancer) did not meet primary endpoints. Development by Telik, Inc. was halted following negative trial results.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Canfosfamide?
Canfosfamide (TLK286) is an investigational glutathione analog prodrug designed for selective activation by GST Pi-overexpressing tumor cells. It was evaluated in clinical trials for ovarian cancer, non-small cell lung cancer, and other solid tumors. Despite encouraging early results, Phase III trials did not demonstrate sufficient efficacy to support regulatory approval, and development was largely discontinued.
What is Canfosfamide used for?
Canfosfamide is educationally associated with: Colorectal cancer treatment, Ovarian cancer treatment, Tumor-selective cytotoxicity via GST Pi overexpression, Non-small cell lung cancer treatment. Educational only — not medical advice.
How is Canfosfamide administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Canfosfamide?
Reported adverse effects include: Thrombocytopenia, Anemia, Hypotension, Nausea and vomiting, Neutropenia, Fatigue. This list is not exhaustive — consult a qualified clinician.
Who should avoid Canfosfamide?
Recorded contraindications: Hypersensitivity to canfosfamide or its components, Severe bone marrow suppression. Consult a qualified clinician before use.