Disitamab vedotin
Also known as: Aidixi, Disitamab vedotin, HER2‑ADC, RC48, RC48-ADC, 爱地希
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Summary
Disitamab vedotin (RC48‑ADC) is an HER2‑targeted antibody‑drug conjugate approved in China for HER2‑positive gastric and gastro‑esophageal junction adenocarcinoma; under clinical investigation for breast and other solid tumours.
Mechanism of Action
Humanized anti‑HER2 monoclonal antibody (Disitamab) binds HER2, is internalized, and releases the cytotoxic payload monomethyl auristatin E (MMAE) which inhibits tubulin polymerization, causing mitotic arrest and tumor cell death.
Routes of Administration
Goals & Uses
- Treatment of other HER2-expressing solid tumorsOncologyLow
- Treatment of HER2-expressing breast cancerOncologyModerate
- Treatment of HER2-positive urothelial carcinomaOncologyHigh
- HER2‑positive gastric cancerOncologyHigh
- HER2‑positive colorectal cancerOncologyModerate
- Treatment of HER2-overexpressing gastric/gastroesophageal junction adenocarcinomaOncologyHigh
- HER2‑positive breast cancerOncologyModerate
Contraindications
- Hypersensitivity to disitamab vedotin or any componentAllergy/ImmunologyHigh
- Severe hepatic impairment (Child‑Pugh C)Liver DiseaseModerate
- Severe hepatic impairmentOrganModerateLiver function concerns
- Known hypersensitivity to Disitamab vedotin or MMAEAllergyHigh
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
Adverse Effects
- Peripheral neuropathyNeurologicalCommon
- Elevated liver enzymes (AST/ALT)HepatotoxicityCommon
- AlopeciaDermatologicCommonHair loss
- Nausea/vomitingGastrointestinalCommon
- Infusion‑related reactionsGeneralCommon
- NeutropeniaHematologicCommonLow neutrophil count
- FatigueGeneralCommonLow energy or tiredness
- Infusion-related reactionsHypersensitivityUncommon
- Myelosuppression (neutropenia, anemia, thrombocytopenia)HematologicalCommon
Drug Interactions
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine)Moderate
- Strong CYP3A4 inducers (e.g., rifampicin, carbamazepine)Moderate
- P-glycoprotein (P-gp) inhibitorsModerate
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)Moderate
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole)High
- Anticoagulants (e.g., warfarin, DOACs)Low
Population Constraints
- PregnancyReproductive SafetyAbsolute
- Pediatric patientsAgeRelative
- Breastfeeding womenReproductiveAbsolute
- Pediatric patients (<18 y)AgeRelative
- LactationReproductiveRelative
- Patients with pre-existing peripheral neuropathyNeurologicalRelative
- Patients with severe hepatic impairmentHepaticRelative
- Pregnant womenReproductiveAbsolute
Regulatory Status
- CNApprovedApproved: HER2-overexpressing (IHC 2+ or 3+) locally advanced or metastatic gastric or gastroesophageal junction adenocarcinoma previously treated with at least two systemic therapies, HER2-positive (IHC 2+ or 3+) locally advanced or metastatic urothelial carcinomaApproved by NMPA (National Medical Products Administration) in June 2021 (gastric cancer) and 2023 (urothelial carcinoma).
- European UnionInvestigationalUnder EMA review; clinical studies ongoing.
- United StatesInvestigationalPhase II/III trials for HER2‑positive gastric and breast cancers.
- United KingdomInvestigationalMHRA has granted clinical trial authorization.
Approved by the National Medical Products Administration (NMPA, China) in 2021. Not yet approved in the US, EU, or UK; currently in Phase II/III trials in those regions.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Disitamab vedotin?
Disitamab vedotin (RC48‑ADC) is an HER2‑targeted antibody‑drug conjugate approved in China for HER2‑positive gastric and gastro‑esophageal junction adenocarcinoma; under clinical investigation for breast and other solid tumours.
What is Disitamab vedotin used for?
Disitamab vedotin is educationally associated with: Treatment of other HER2-expressing solid tumors, Treatment of HER2-expressing breast cancer, Treatment of HER2-positive urothelial carcinoma, HER2‑positive gastric cancer, HER2‑positive colorectal cancer, Treatment of HER2-overexpressing gastric/gastroesophageal junction adenocarcinoma, HER2‑positive breast cancer. Educational only — not medical advice.
How is Disitamab vedotin administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Disitamab vedotin?
Reported adverse effects include: Peripheral neuropathy, Elevated liver enzymes (AST/ALT), Alopecia, Nausea/vomiting, Infusion‑related reactions, Neutropenia, Fatigue, Infusion-related reactions, Myelosuppression (neutropenia, anemia, thrombocytopenia). This list is not exhaustive — consult a qualified clinician.
Who should avoid Disitamab vedotin?
Recorded contraindications: Hypersensitivity to disitamab vedotin or any component, Severe hepatic impairment (Child‑Pugh C), Severe hepatic impairment, Known hypersensitivity to Disitamab vedotin or MMAE, Pregnancy. Consult a qualified clinician before use.