Disitamab Vedotin
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Summary
Disitamab Vedotin (CHEMBL5095273) is a phase-3 clinical-stage antibody drug conjugate targeting ERBB2; indicated across 11 conditions including urothelial carcinoma and breast neoplasm; with CIViC clinical evidence for 1 variant-indication association (e.g. ERBB2 Amplification AND CDK12 Amplification in breast cancer).
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Antibody drug conjugate
- Targets: 1 (ERBB2)
- Indications: 11 conditions
- Clinical trials: 53
- Precision-oncology evidence (CIViC): 1 variant–indication association
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL5095273 |
| Name | Disitamab Vedotin |
| Type | Antibody drug conjugate |
| Max phase | 3 |
Also known as: Disitamab vedotin, DISITAMAB VEDOTIN
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| ERBB2 | erb-b2 receptor tyrosine kinase 2 | Inhibition | 17.7% | P04626 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): ERBB2.
Top Reactome pathways
33 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signaling by ERBB2 | 1 | ERBB2 |
| SHC1 events in ERBB2 signaling | 1 | ERBB2 |
| PLCG1 events in ERBB2 signaling | 1 | ERBB2 |
| PIP3 activates AKT signaling | 1 | ERBB2 |
| GRB7 events in ERBB2 signaling | 1 | ERBB2 |
| Downregulation of ERBB2:ERBB3 signaling | 1 | ERBB2 |
| GRB2 events in ERBB2 signaling | 1 | ERBB2 |
| PI3K events in ERBB2 signaling | 1 | ERBB2 |
| Constitutive Signaling by Aberrant PI3K in Cancer | 1 | ERBB2 |
| Sema4D induced cell migration and growth-cone collapse | 1 | ERBB2 |
| RAF/MAP kinase cascade | 1 | ERBB2 |
| ERBB2 Regulates Cell Motility | 1 | ERBB2 |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 1 | ERBB2 |
| ERBB2 Activates PTK6 Signaling | 1 | ERBB2 |
| Downregulation of ERBB2 signaling | 1 | ERBB2 |
| TFAP2 (AP-2) family regulates transcription of growth factors and their receptors | 1 | ERBB2 |
| Constitutive Signaling by Overexpressed ERBB2 | 1 | ERBB2 |
| Drug-mediated inhibition of ERBB2 signaling | 1 | ERBB2 |
| Signaling by ERBB2 KD Mutants | 1 | ERBB2 |
| Resistance of ERBB2 KD mutants to trastuzumab | 1 | ERBB2 |
| Resistance of ERBB2 KD mutants to sapitinib | 1 | ERBB2 |
| Resistance of ERBB2 KD mutants to tesevatinib | 1 | ERBB2 |
| Resistance of ERBB2 KD mutants to neratinib | 1 | ERBB2 |
| Resistance of ERBB2 KD mutants to osimertinib | 1 | ERBB2 |
| Resistance of ERBB2 KD mutants to afatinib | 1 | ERBB2 |
| Resistance of ERBB2 KD mutants to AEE788 | 1 | ERBB2 |
| Resistance of ERBB2 KD mutants to lapatinib | 1 | ERBB2 |
| Signaling by ERBB2 ECD mutants | 1 | ERBB2 |
| Signaling by ERBB2 TMD/JMD mutants | 1 | ERBB2 |
| Drug resistance in ERBB2 TMD/JMD mutants | 1 | ERBB2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 1 |
| signal transduction | 1 |
| cell surface receptor signaling pathway | 1 |
| enzyme-linked receptor protein signaling pathway | 1 |
| cell surface receptor protein tyrosine kinase signaling pathway | 1 |
| epidermal growth factor receptor signaling pathway | 1 |
| heart development | 1 |
| neuromuscular junction development | 1 |
| motor neuron axon guidance | 1 |
| cell population proliferation | 1 |
| Schwann cell development | 1 |
| peptidyl-tyrosine phosphorylation | 1 |
| neuron differentiation | 1 |
| positive regulation of cell growth | 1 |
| regulation of microtubule-based process | 1 |
Indications & clinical
Indications
11 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| urothelial carcinoma | 3 | MONDO:0040679 | EFO:0008528 |
| breast neoplasm | 3 | MONDO:0021100 | MONDO:0007254 |
| colorectal neoplasm | 2 | MONDO:0005335 | EFO:0004142 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| neoplasm | 1 | MONDO:0005070 | EFO:0000616 |
5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 53.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 34 |
| PHASE3 | 5 |
| Not specified | 5 |
| PHASE1/PHASE2 | 3 |
| PHASE4 | 2 |
| PHASE2/PHASE3 | 2 |
| PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05488353 | PHASE4 | UNKNOWN | A Clinical Study of Disitamab Vedotin for Injection Combined With Penpulimab Injection in Neoadjuvant Therapy for Patients With HER2-expressing Cisplatin-intolerant cT2-T4aNxM0 Bladder Urothelial Carcinoma |
| NCT05723991 | PHASE4 | UNKNOWN | Study of Disitamab Vedotin Combined With Gemcitabine in Neoadjuvant Treatment of Urothelial Carcinoma |
| NCT05904964 | PHASE3 | RECRUITING | Disitamab Vedotin (RC48) in Hormone Receptor Positive, HER2-low Metastatic Breast Cancer (the Rosy Trial) |
| NCT05911295 | PHASE3 | ACTIVE_NOT_RECRUITING | Disitamab Vedotin With Pembrolizumab vs Chemotherapy in Previously Untreated Urothelial Cancer Expressing HER2 |
| NCT06278870 | PHASE3 | RECRUITING | Disitamab Vedotin + Pyrotinib Versus THP in the First-line Treatment for HER2+ Advanced Breast Cancer Clinical Trial |
| NCT06944496 | PHASE3 | NOT_YET_RECRUITING | A Study of Disitamab Vedotin Combined With Tislelizumab and Chemotherapy Versus Tislelizumab Combined With Chemotherapy in HER2-Low Advanced Gastric or Gastroesophageal Junction Adenocarcinoma |
| NCT07315750 | PHASE3 | RECRUITING | A Study of Disitamab Vedotin Combined With Trastuzumab and Tislelizumab Versus Chemotherapy Combined With Trastuzumab With or Without Pembrolizumab in HER2-high Expression Advanced Gastric or Gastroesophageal Junction Adenocarcinoma. |
| NCT07366840 | PHASE2/PHASE3 | NOT_YET_RECRUITING | RC48 Combined With Chemotherapy in HER2-Positive Advanced Breast Cancer Patients With Prior TOP1i-ADC Failure |
| NCT07608224 | PHASE2/PHASE3 | NOT_YET_RECRUITING | HOPE-07-MIBC: Disitamab Vedotin Plus Immunotherapy vs Chemoimmunotherapy in Resectable HER2-Expressing MIBC |
| NCT04879329 | PHASE2 | RECRUITING | A Study of Disitamab Vedotin Alone or With Pembrolizumab in Urothelial Cancer That Expresses HER2 |
| NCT05586061 | PHASE2 | ACTIVE_NOT_RECRUITING | First-line Treatment with RC48 Plus Tislelizumab and S-1(RCTS) in Advanced Gastric Cancer |
| NCT05912205 | PHASE2 | NOT_YET_RECRUITING | Disitamab Vedotin Combined With Radiotherapy for Bladder Preservation |
| NCT06003231 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study of Disitamab Vedotin in Previously Treated Solid Tumors That Express HER2 |
| NCT06155383 | PHASE2 | RECRUITING | Perioperative Disitamab Vedotin Plus Toripalimab and XELOX in Gastric or Gastroesophageal Junction Adenocarcinoma. |
| NCT06155396 | PHASE2 | RECRUITING | A Study of RC48-ADC Combination With Zimberelimab Injection Therapies at Least First-line Platinum-containing Standard Therapy Failed With Recurrent or Metastatic Cervical Cancer |
| NCT06157892 | PHASE2 | RECRUITING | A Study of Disitamab Vedotin With Other Anticancer Drugs in Solid Tumors |
| NCT06185400 | PHASE2 | NOT_YET_RECRUITING | RC48 Combined With EGFR or HER2 TKI for Locally Advanced or Metastatic NSCLC Patients With HER2 Alterations |
| NCT06187506 | PHASE2 | RECRUITING | Disitamab Vedotin Combined With BCG Therapy in HER2-expressing High-risk Non-muscle Invasive Bladder Cancer |
| NCT06210490 | PHASE2 | RECRUITING | A Clinical Study of the Efficacy and Safety of Disitamab Vedotin in Combination With Radiotherapy for the Adjuvant Treatment of HER2 Overexpressing UTUC Patients With High Risk Factors for Recurrence After Radical Surgery |
| NCT06378242 | PHASE1/PHASE2 | RECRUITING | To Evaluate the Safety, Efficacy, and Pharmacokinetics of Intravesical Instiliations of Disitamab Vedotin in Patients With High-risk Non-muscular Invasive Bladder Cancer (NMIBC) That Express HER2 |
| NCT06389006 | PHASE2 | RECRUITING | To Evaluate the Efficacy and Safety of Disitamab Vedotin Combined With Toripalimab Sequential Chemotherapy as Neoadjuvant Treatment in Patients With HR-positive, HER2-low Breast Cancer |
| NCT06492317 | PHASE2 | NOT_YET_RECRUITING | RC48 Plus AK104 as First-line Treatment for HER2-overexpressing Advanced Gastric Cancer |
| NCT06642545 | PHASE2 | RECRUITING | Efficacy and Safety Study of Disitamab Vedotin + RC148 vs. Albumin-Paclitaxone ± Toripalimab in HR-/HER2-low Breast Cancer |
| NCT06650332 | PHASE1/PHASE2 | RECRUITING | Cadonilimab Combination Regimen as First-line Treatment for HER2-expressing GC/GEJ Patients |
| NCT06730373 | PHASE2 | RECRUITING | First-line Treatment With RC48 Plus Sintilimab and S-1 in Advanced Gastric Cancer (RCTS2) |
| NCT06734182 | PHASE2 | RECRUITING | Neoadjuvant Envafolimab Plus Disitamab Vedotin and Carboplatin in Resectable HER2-Mutant Non-Small-Cell Lung Cancer |
| NCT06749860 | PHASE2 | RECRUITING | Disitamab Vedotin in Combination with Tislelizumab and Bevacizumab in a Phase II Clinical Study of Locally Advanced or Metastatic Non-small Cell Lung Cancer with HER2 Mutation/amplification/expression |
| NCT06904573 | PHASE2 | RECRUITING | Probiotics in Advanced Urothelial Carcinoma |
| NCT06966453 | PHASE1/PHASE2 | RECRUITING | A Study of Disitamab Vedotin in Adults With HER2 Expressing Advanced Breast Cancer |
| NCT07065435 | PHASE2 | RECRUITING | RC48 Plus Bevacizumab or Pyrotinib in HER2-Positive Metastatic Breast Cancer After T-DXd Failure: A Phase II Study |
| NCT07093866 | PHASE2 | RECRUITING | Efficacy and Safety of Disitamab Vedotin Plus Abiraterone for Metastatic Castration-Resistant Prostate Cancer：a Phase II Study |
| NCT07142200 | PHASE2 | NOT_YET_RECRUITING | A Clinical Study Evaluating the Efficacy and Safety of Disitamab Vedotin Combined With PD-1 Inhibitor and Radiotherapy as Bladder-preserving Therapy in Patients With Localized HER2-high Expressing Muscle-invasive Bladder Urothelial Carcinoma Following Maximal Transurethral Resection |
| NCT07159217 | PHASE2 | NOT_YET_RECRUITING | Disitamab Vedotin Plus Lenvatinib and PD-1 Inhibitors for Treating HER2-positive Advanced Biliary Tract Cancer |
| NCT07446452 | PHASE2 | RECRUITING | Disitamab Vedotin Plus Bevacizumab in HER2-Low Metastatic Breast Cancer After T-DXd Failure: A Phase II Study |
| NCT07474064 | PHASE2 | NOT_YET_RECRUITING | Probiotics Combined With Targeted Therapy Plus Immunotherapy in Bladder-Preserving Setting for Patients With MIBC |
| NCT07498907 | PHASE2 | NOT_YET_RECRUITING | Disitamab Vedotin Plus Radiotherapy for Adjuvant Treatment of HER2-Expressing Cisplatin-Ineligible Upper Tract Urothelial Carcinoma |
| NCT07509424 | PHASE2 | NOT_YET_RECRUITING | Neoadjuvant Short-course Radiotherapy Followed by a Combination of Disitamab Vedotin, Sintilimab, and Capecitabine in Locally Advanced HER2-expressing Rectal Cance |
| NCT05333809 | PHASE2 | UNKNOWN | Pembrolizumab and Disitamab Vedotin in HER2-expressing Metastatic Colorectal Cancer |
| NCT05493683 | PHASE2 | UNKNOWN | Disitamab Vedotin Combined With Tislelizumab in Advanced HER2 Positive Colorectal Cancer |
| NCT05495724 | PHASE2 | UNKNOWN | Disitamab Vedotin Combined With Tislelizumab for Her2 Overexpressing High-Risk Non-Muscle-Invasive Urothelial Bladder Carcinoma Which is Not Completely Resectable |
Clinical evidence (CIViC)
Variant × indication × effect (1 predictive associations from 1 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| ERBB2 Amplification AND CDK12 Amplification | Breast Cancer | Sensitivity/Response | Trastuzumab Deruxtecan Regimen + Trastuzumab Emtansine Regimen + Disitamab Vedotin | CIViC B | EID12569 |
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
86 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | ERBB2 |
| DACOMITINIB | ChEMBL + PubChem | Phase 4 (approved) | ERBB2 |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | ERBB2 |
| LAPATINIB DITOSYLATE | ChEMBL + PubChem | Phase 4 (approved) | ERBB2 |
| LAZERTINIB | ChEMBL + PubChem | Phase 4 (approved) | ERBB2 |
| MOBOCERTINIB | ChEMBL + PubChem | Phase 4 (approved) | ERBB2 |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| AFATINIB DIMALEATE | ChEMBL | Phase 4 (approved) | ERBB2 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | ERBB2 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | ERBB2 |
| BITHIONOL | ChEMBL | Phase 4 (approved) | ERBB2 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | ERBB2 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | ERBB2 |
| COLISTIN | ChEMBL | Phase 4 (approved) | ERBB2 |
| DASATINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| DOXORUBICIN | ChEMBL | Phase 4 (approved) | ERBB2 |
| EBASTINE | ChEMBL | Phase 4 (approved) | ERBB2 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | ERBB2 |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | ERBB2 |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | ERBB2 |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| IMATINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| LAPATINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | ERBB2 |
| MITOXANTRONE | ChEMBL | Phase 4 (approved) | ERBB2 |
| NERATINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| PACLITAXEL | ChEMBL | Phase 4 (approved) | ERBB2 |
| PONATINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| SORAFENIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| TAMOXIFEN | ChEMBL | Phase 4 (approved) | ERBB2 |
| TIRABRUTINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| TRIBROMSALAN | ChEMBL | Phase 4 (approved) | ERBB2 |
| TUCATINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| VANDETANIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| ZANUBRUTINIB | ChEMBL | Phase 4 (approved) | ERBB2 |
| ALISERTIB | ChEMBL | Phase 3 | ERBB2 |
| ALVOCIDIB | ChEMBL | Phase 3 | ERBB2 |
| CANDESARTAN | ChEMBL | Phase 3 | ERBB2 |
| CANERTINIB | ChEMBL | Phase 3 | ERBB2 |
| CEDIRANIB | ChEMBL | Phase 3 | ERBB2 |
| ENCLOMIPHENE | ChEMBL | Phase 3 | ERBB2 |
| MASITINIB | ChEMBL | Phase 3 | ERBB2 |
| POZIOTINIB | ChEMBL | Phase 3 | ERBB2 |
| PYROTINIB | ChEMBL | Phase 3 | ERBB2 |
| REMIBRUTINIB | ChEMBL | Phase 3 | ERBB2 |
| TANESPIMYCIN | ChEMBL | Phase 3 | ERBB2 |
| ZONGERTINIB | ChEMBL | Phase 3 | ERBB2 |
| AEE-788 | ChEMBL | Phase 2 | ERBB2 |
| ALLITINIB | ChEMBL | Phase 2 | ERBB2 |
| ATUZABRUTINIB | ChEMBL | Phase 2 | ERBB2 |
| BENZETHONIUM CHLORIDE | ChEMBL | Phase 2 | ERBB2 |
| CENISERTIB | ChEMBL | Phase 2 | ERBB2 |
| CLOSANTEL | ChEMBL | Phase 2 | ERBB2 |
| CP-724714 | ChEMBL | Phase 2 | ERBB2 |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | ERBB2 |
Related Atlas pages
- Genes: ERBB2
- Diseases: urothelial carcinoma, breast neoplasm, breast carcinoma
- Drugs: Afatinib, Dacomitinib, Gefitinib, Lapatinib Ditosylate, Lazertinib, Mobocertinib, Acalabrutinib, Amiodarone, Astemizole, Bithionol, Bosutinib, Brigatinib, Cabozantinib, Chlorpromazine, Clotrimazole, Colistin, Dasatinib, Doxorubicin, Ebastine, Econazole, Erlotinib, Fluphenazine, Hexachlorophene, Ibrutinib, Imatinib, Miconazole, Mitoxantrone, Neratinib, Osimertinib, Paclitaxel, Ponatinib, Sorafenib, Tamoxifen, Tirabrutinib, Tribromsalan, Tucatinib, Vandetanib, Zanubrutinib, Alisertib, Alvocidib, Candesartan, Canertinib, Cediranib, Enclomiphene, Masitinib, Poziotinib, Pyrotinib, Remibrutinib, Tanespimycin, Zongertinib