Zoptarelin doxorubicin
Also known as: AEZS-108, AN-152, D-Lys6-LHRH-doxorubicin, Zoptarelin doxorubicin, Zoptrex
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Summary
Zoptarelin doxorubicin (AEZS‑108) is a peptide‑drug conjugate that couples an LHRH agonist to the anthracycline doxorubicin for targeted chemotherapy of LHRH‑receptor‑positive cancers.
Mechanism of Action
Binds LHRH receptors on tumor cells, internalizes, and releases doxorubicin which intercalates DNA and inhibits topoisomerase II, leading to cytotoxicity.
Routes of Administration
Goals & Uses
- Targeted cytotoxic deliveryEfficacyModerate
- Reduction of systemic doxorubicin toxicity via tumor targetingToxicity ReductionModerate
- Targeted treatment of ovarian cancerOncologyLow
- Targeted treatment of LHRH receptor-positive endometrial cancerOncologyModerate
- Treatment of LHRH‑positive solid tumorsIndicationModerate
- Targeted treatment of castration-resistant prostate cancerOncologyLow
- Reduced systemic cardiotoxicitySafetyModerate
Contraindications
- Severe pre-existing cardiomyopathy or heart failureCardiovascularHigh
- Known hypersensitivity to doxorubicinAllergyHigh
- Severe hepatic impairmentOrganModerateLiver function concerns
- Hypersensitivity to doxorubicin or LHRH analoguesAllergyHigh
- Pregnancy or lactationReproductiveHigh
- Severe cardiac dysfunction (ejection fraction < 50%)CardiacHigh
- Cumulative anthracycline dose at or near maximum lifetime limitOncologyHigh
Adverse Effects
- CardiotoxicityCardiovascularUncommon
- AlopeciaDermatologicCommonHair loss
- Hot flashesEndocrine / VasomotorUncommon
- Nausea/vomitingGastrointestinalCommon
- Hot flashes / hormonal effectsEndocrineUncommon
- Fatigue and astheniaConstitutionalCommon
- Nausea and vomitingGastrointestinalCommon
- MyelosuppressionHematologicCommon
- Myelosuppression (neutropenia, anemia, thrombocytopenia)HematologicalCommon
Drug Interactions
- Anticoagulants (e.g., warfarin)Moderate
- Live vaccinesHigh
- CYP3A4 inhibitors (e.g., ketoconazole)Moderate
- Other anthracyclinesHigh
- Other anthracyclines or cardiotoxic agentsHigh
- CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)Moderate
Population Constraints
- PregnancyReproductive SafetyAbsolute
- Pediatric patientsAgeRelative
- Patients with LHRH receptor-negative tumorsBiomarkerRelative
- BreastfeedingReproductiveAbsolute
- Elderly (>75 years)GeriatricRelative
Regulatory Status
- European UnionInvestigationalNo EMA marketing authorization.
- United StatesInvestigationalPhase II/III trials discontinued; not FDA approved.
- United KingdomInvestigationalNot MHRA approved.
Completed Phase II trials; Phase III discontinued; not approved in major jurisdictions.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Zoptarelin doxorubicin?
Zoptarelin doxorubicin (AEZS‑108) is a peptide‑drug conjugate that couples an LHRH agonist to the anthracycline doxorubicin for targeted chemotherapy of LHRH‑receptor‑positive cancers.
What is Zoptarelin doxorubicin used for?
Zoptarelin doxorubicin is educationally associated with: Targeted cytotoxic delivery, Reduction of systemic doxorubicin toxicity via tumor targeting, Targeted treatment of ovarian cancer, Targeted treatment of LHRH receptor-positive endometrial cancer, Treatment of LHRH‑positive solid tumors, Targeted treatment of castration-resistant prostate cancer, Reduced systemic cardiotoxicity. Educational only — not medical advice.
How is Zoptarelin doxorubicin administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Zoptarelin doxorubicin?
Reported adverse effects include: Cardiotoxicity, Alopecia, Hot flashes, Nausea/vomiting, Hot flashes / hormonal effects, Fatigue and asthenia, Nausea and vomiting, Myelosuppression, Myelosuppression (neutropenia, anemia, thrombocytopenia). This list is not exhaustive — consult a qualified clinician.
Who should avoid Zoptarelin doxorubicin?
Recorded contraindications: Severe pre-existing cardiomyopathy or heart failure, Known hypersensitivity to doxorubicin, Severe hepatic impairment, Hypersensitivity to doxorubicin or LHRH analogues, Pregnancy or lactation, Severe cardiac dysfunction (ejection fraction < 50%), Cumulative anthracycline dose at or near maximum lifetime limit. Consult a qualified clinician before use.