Rivoceranib
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Rivoceranib
- Molecular weight
- 397.48
- Structure (SMILES)
- N#CC1(c2ccc(NC(=O)c3cccnc3NCc3ccncc3)cc2)CCCC1
- apatinib
- Apatinib
- apatinib free base
- Apatinib free base
- rivoceranib
- Rivoceranib
- rivoceranib [INN]
- RIVOCERANIB [USAN]
- Rivoceranib [WHO-DD]
- rivoceranib inn
- rivoceranib usan
- rivoceranib who dd
- yn968d1
- YN968D1
- yn968d1 free base
- YN968D1 FREE BASE
- CAS registry numbers
- 811803-05-1
- ChEMBL ID
- CHEMBL3186534
- InChIKey
- WPEWQEMJFLWMLV-UHFFFAOYSA-N
- PubChem compound IDs
- 11315474
- FDA ingredient codes (UNII)
- 5S371K6132
- Patents
- 0
- Designations
- 2
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Pharmacology name
- rivoceranib
- Type
- Synthetic organic
- Drug name stem
- -anib
- Approval recorded by Guide to Pharmacology
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- ret proto-oncogene
- Gene symbol
- RET
- Protein identifier
- P07949
- Median affinity
- 7.89
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- KIT proto-oncogene, receptor tyrosine kinase
- Gene symbol
- KIT
- Protein identifier
- P10721
- Median affinity
- 6.37
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- kinase insert domain receptor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Median affinity
- 9
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- C-terminal Src kinase
- Gene symbol
- CSK
- Protein identifier
- P41240
- Median affinity
- 6.28
- Affinity units
- pIC50
Open Targets mechanisms
- Mechanism
- Vascular endothelial growth factor receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor 2
- Action type
- Inhibitor
- Gene symbol
- RET
- Protein identifier
- P07949
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- KIT
- Protein identifier
- P10721
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- SRC
- Protein identifier
- P12931
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- CSK
- Protein identifier
- P41240
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000178
- Subject identifier
- D013274
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Squamous Cell Carcinoma of Head and Neck
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000199
- Subject identifier
- D000077195
- Condition
- Lymphoma, T-Cell, Peripheral
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000211
- Subject identifier
- D016411
- Condition
- Carcinoma, Adenoid Cystic
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000231
- Subject identifier
- D003528
- Condition
- Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000503
- Subject identifier
- D013274
- Condition
- Adenocarcinoma of Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000571
- Subject identifier
- D000077192
- Condition
- Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Neuroblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000621
- Subject identifier
- D009447
- Condition
- Osteosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Sarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000691
- Subject identifier
- D012509
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000707
- Subject identifier
- D002294
- Condition
- Melanoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Uterine Cervical Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001061
- Subject identifier
- D002583
- Condition
- Lung Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001071
- Subject identifier
- D008175
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002892
- Subject identifier
- D013964
- Condition
- Esophageal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002916
- Subject identifier
- D004938
- Condition
- Medulloblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002939
- Subject identifier
- D008527
And 41 more, listed on the interactive page.
- Condition identifier
- EFO_0000178
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000231
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000503
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000571
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000574
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000621
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000637
- Condition identifier
- EFO_0000681
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000691
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000702
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000707
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 3
- Condition identifier
- EFO_0001061
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001071
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002916
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002939
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003860
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003868
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003869
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003891
- Highest recorded phase
- 2
And 114 more, listed on the interactive page.
- Event
- alanine aminotransferase increased
- Reports
- 6
- Reporting signal score
- 12.1393
- Event
- anaemia
- Reports
- 16
- Reporting signal score
- 34.5547
- Event
- aspartate aminotransferase increased
- Reports
- 5
- Reporting signal score
- 9.76738
- Event
- bone marrow failure
- Reports
- 9
- Reporting signal score
- 31.2267
- Event
- cortisol abnormal
- Reports
- 1
- Reporting signal score
- 7.05557
- Event
- decreased appetite
- Reports
- 9
- Reporting signal score
- 17.0074
- Event
- diarrhoea
- Reports
- 12
- Reporting signal score
- 12.7575
- Event
- disease progression
- Reports
- 5
- Reporting signal score
- 8.69594
- Event
- drug resistance
- Reports
- 6
- Reporting signal score
- 18.2272
- Event
- fatigue
- Reports
- 11
- Reporting signal score
- 10.1693
- Event
- gastrointestinal disorder
- Reports
- 4
- Reporting signal score
- 8.08631
- Event
- gastrointestinal toxicity
- Reports
- 2
- Reporting signal score
- 7.24709
- Event
- haemorrhage
- Reports
- 6
- Reporting signal score
- 12.5851
- Event
- hyperbilirubinaemia
- Reports
- 4
- Reporting signal score
- 13.7782
- Event
- hypertension
- Reports
- 18
- Reporting signal score
- 44.1652
- Event
- hypoalbuminaemia
- Reports
- 3
- Reporting signal score
- 10.566
- Event
- hypothyroidism
- Reports
- 7
- Reporting signal score
- 23.1451
- Event
- leukopenia
- Reports
- 14
- Reporting signal score
- 44.483
- Event
- liposarcoma recurrent
- Reports
- 1
- Reporting signal score
- 8.47671
- Event
- myelosuppression
- Reports
- 4
- Reporting signal score
- 13.6372
- Event
- neurotoxicity
- Reports
- 3
- Reporting signal score
- 7.84555
- Event
- neutropenia
- Reports
- 9
- Reporting signal score
- 16.372
- Event
- palmar-plantar erythrodysaesthesia syndrome
- Reports
- 13
- Reporting signal score
- 51.1608
- Event
- pneumonitis
- Reports
- 3
- Reporting signal score
- 7.2006
- Event
- proteinuria
- Reports
- 11
- Reporting signal score
- 43.1342
And 6 more, listed on the interactive page.
- NCT00633490
- NCT04282278
- NCT04428086
- NCT04569916
- NCT04832204
- NCT00970138
- NCT02409199
- NCT03355612
- NCT03599778
- NCT01176669
- NCT02768415
- NCT02878057
- NCT03086785
- NCT03254654
- NCT03348098
- NCT03394287
- NCT03457467
- NCT03535961
- NCT03580395
- NCT03735082
- NCT03945604
- NCT03982485
- NCT04296370
- NCT04303741
- NCT04335006
And 261 more, listed on the interactive page.
- Hydrogen bond acceptors
- 5
- Hydrogen bond donors
- 2
- Polar surface area
- 90.7
- Calculated partition coefficient (ALogP)
- 4.68
- Calculated partition coefficient (XLogP)
- 4.1
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 6
- Heavy atoms
- 30
- Molecular formula
- C24H23N5O
- Monoisotopic mass
- 397.19026037
- Natural product
- No
- Recorded assays
- 717
- Active assays
- 30
- Confirmatory
- Other
- Screening
- Antineoplastic Agents
Substances that inhibit or prevent the proliferation of NEOPLASMS.
- Protein Kinase Inhibitors
Agents that inhibit PROTEIN KINASES.
Related records
Trials (430)
- A Clinical Study of Adebrelimab Combined With Apatinib and Paclitaxel in Patients With Advanced Gastric Cancer.
- A Clinical Study of Apatinib in Patients With Local Progressive/Metastatic Refractory Thyroid Cancer
- A Clinical Study of Exploring Camrelizumab in the Treatment of Colorectal Mucinous Adenocarcinoma(MAC)
- A Clinical Study To Evaluate Camrelizumab (SHR-1210) Plus Capecitabine and Oxaliplatin Followed by Sequential Treatment With Camrelizumab Plus Apatinib Mesylate in Advanced or Metastatic Gastric Cancer (GC) or Gastroesophageal Junction Cancer (GEJ) Without Prior Systemic Therapy
- A Clinical Trial of Apatinib Plus Docetaxel in Locally Advanced or Metastatic Gastric or GEJ Adenocarcinoma
- A Clinical Trial With Apatinib for Subjects With Refractory Malignant Ascites
- A LM-302 Combination With Other Anti-Tumor Therapies Phase ll Study
- A One-arm Exploratory Clinical Research Program Study of Apatinib in Advanced Metastatic Renal Cell Carcinoma Patients.
- A One-Arm Exploratory Clinical Trial of Apatinib Plus Gemcitabine in Patients With Advanced Metastatic Pancreatic Cancer
- A Pharmacokinetic Interaction Study Between Apatinib and Rosuvastatin or Metformin in Solid Tumor Subjects.
- A Phase 2 Trial of Fluzoparib Combined With Apatinib Versus Fluzoparib Monotherapy in Treatment With Relapsed Ovarian Cancer Patients
- A Phase 3 Study Comparing Carelizumab Plus Nab-paclitaxel and Apatinib, Carelizumab Plus Nab-paclitaxel, and Nab-paclitaxel in Patients With Advanced Triple Negative Breast Cancer.
- A Phase Ib/II Clinical Study of Camrelizumab and Apatinib Plus GP in the Treatment of Advanced Biliary Tract Cancer
- A Phase II Exploratory Clinical Trial of Multiple Drug Combinations in the Treatment of Advanced Esophageal Squamous Cell Carcinoma
- A Phase II Study of Apatinib in STS Patients
- A Phase II Study of Carelizumab Combined With Irinotecan and Apatinib of Second-line Treatment for Advanced Gastric Cancer
- A Phase II Study of Rivoceranib for Patients With Recurrent or Metastatic Olfactory Neuroblastoma
- A Phase II Trial of Camrelizumab in Combination With Apatinib and Eribulin in Patients With Advanced TNBC
- A Phase III Randomized Study of TACE Plus an Oral Triple-Agent Cocktail Versus TACE Plus First-Line Targeted Immunotherapy in Unresectable Hepatocellular Carcinoma
- A Prospective Study of Apatinib Plus Concurrent Neoadjuvant Chemoradiotherapy for Siewert II ，III of Locally Advanced HER-2 Negative Adenocarcinoma at Gastroesophageal Junction
In development for (70)
- Adenoid cystic carcinoma Phase 2
- Biliary tract cancer Phase 2
- Biliary tract neoplasm Phase 2
- Breast cancer Phase 3
- Breast neoplasm Phase 3
- Cancer Phase 2
- Carcinoma Phase 2
- Carcinoma of esophagus Phase 3
- Cervical cancer Phase 2
- Cervical carcinoma Phase 2
- Cholangiocarcinoma Phase 2
- Colorectal adenocarcinoma Phase 3
- Colorectal cancer Phase 3
- Colorectal neoplasm Phase 3
- Digestive system cancer Phase 2
- Esophageal cancer Phase 3
- Esophageal squamous cell carcinoma Phase 3
- Exocrine pancreatic carcinoma Phase 2
- Gallbladder carcinoma Phase 2
- Gastric adenocarcinoma Phase 3
Other linked conditions (1)
- Non-small cell squamous lung carcinoma
Targets (1)
- KDR Vascular endothelial growth factor receptor 2 inhibitor