Rivoceranib mesylate
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 mesylate
- Molecular weight
- 493.59
- Structure (SMILES)
- CS(=O)(=O)O.N#CC1(c2ccc(NC(=O)c3cccnc3NCc3ccncc3)cc2)CCCC1
- aitan
- Aitan
- Apatinib (registered name in China)
- apatinib mesylate
- Apatinib mesylate
- apatinib registered name in china
- rivoceranib mesylate
- Rivoceranib mesylate
- RIVOCERANIB MESYLATE [USAN]
- Rivoceranib mesylate [WHO-DD]
- rivoceranib mesylate usan
- rivoceranib mesylate who dd
- yn 968d1
- Yn-968d1
- YN-968D1
- yn968d1
- YN968D1
- CAS registry numbers
- 1218779-75-9
- ChEMBL ID
- CHEMBL3545414
- InChIKey
- FYJROXRIVQPKRY-UHFFFAOYSA-N
- PubChem compound IDs
- 45139106
- FDA ingredient codes (UNII)
- TK02X14ASJ
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Drug name stem
- -anib
Mechanisms of action
- Mechanism
- Vascular endothelial growth factor receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor 2
- Protein identifier
- P35968
Open Targets mechanisms
- Mechanism
- Vascular endothelial growth factor receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor 2
- 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
- Carcinoma, Adenoid Cystic
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000231
- Subject identifier
- D003528
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000503
- Subject identifier
- D013274
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Osteosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004142
- Subject identifier
- D015179
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Esophageal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005922
- Subject identifier
- D004938
- Condition
- Sarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001968
- Subject identifier
- D012509
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1002017
- Subject identifier
- D013964
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0001056
- Subject identifier
- D013274
- Condition
- Adenocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0003219
- Subject identifier
- D000230
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0008170
- Subject identifier
- D010051
- Condition
- Nasopharyngeal Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0015459
- Subject identifier
- D000077274
- 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
- 2
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000702
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- EFO_0004142
- Condition identifier
- EFO_0005922
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001968
- Highest recorded phase
- 2
- Condition identifier
- EFO_1002017
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001056
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0003219
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003220
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Condition identifier
- MONDO_0005036
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005072
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005140
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005494
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005580
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0007254
And 10 more, listed on the interactive page.
- Event
- bronchial fistula
- Reports
- 1
- Reporting signal score
- 7.10737
- Event
- cytokine increased
- Reports
- 1
- Reporting signal score
- 11.4178
- Event
- hyperthyroidism
- Reports
- 2
- Reporting signal score
- 7.16617
- Event
- myelosuppression
- Reports
- 3
- Reporting signal score
- 12.4013
- Event
- palmar-plantar erythrodysaesthesia syndrome
- Reports
- 6
- Reporting signal score
- 25.0399
- Event
- pneumonitis
- Reports
- 3
- Reporting signal score
- 10.2223
- Event
- proteinuria
- Reports
- 7
- Reporting signal score
- 31.7381
- Event
- secondary hypertension
- Reports
- 5
- Reporting signal score
- 41.8112
- NCT01497704
- NCT01726101
- NCT02711969
- NCT03219593
- NCT04006821
- NCT04089657
- NCT04195828
- NCT04338438
- NCT04342910
- NCT04345783
- NCT04714190
- NCT05025033
- NCT05223088
- NCT05524974
- NCT02772029
- NCT04523662
- NCT04850040
- NCT04930315
- NCT05320692
- NCT05613478
- NCT02775370
- NCT02836171
- NCT02836821
- NCT04322552
- NCT04457180
And 36 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
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 6
- Heavy atoms
- 35
- Molecular formula
- C25H27N5O4S
- Monoisotopic mass
- 493.17837553
- Natural product
- No
- Recorded assays
- 12
- Active assays
- 1
Active assay types
- Confirmatory
- Antineoplastic Agents
- Protein Kinase Inhibitors
Related records
Trials (89)
- A Clinical Trial of Maintenance Treatment of Apatinib in Advanced Gastric Cancer Patients Have Completed Postoprative Adjuvant Chemotherapy
- A Food Effect Study of Apatinib Mesylate in Healthy Subjects
- A Multicenter Clinical Study of Apatinib Mesylate Combined With Doctor's Choice for Advanced Breast Cancer
- A Multicenter, Randomized, Open-label, Controlled Study of HAIC Combined With Camrelizumab and Apatinib Mesylate for Perioperative Treatment of Resectable Hepatocellular Carcinoma With High-risk Recurrence Factors
- A Neoadjuvant Hepatocellular Carcinoma Study of Camrelizumab in Combination With Apatinib and Oxaliplatin
- A Pharmacokinetic Interaction Study Between Apatinib Mesylate and Repaglinide or Bupropion in Advanced Solid Tumor Subjects
- A Pharmacokinetic Interaction Study Between Apatinib Mesylate and Transporter Pgp Substrate Digoxin in Advanced Solid Tumor Subjects
- A Study of Adebrelimab Combined With Apatinib Mesylate and Chemotherapy for Neoadjuvant Therapy and Biomarker Analysis in Limited-stage Small Cell Lung Cancer
- A Study of Apatinib and Tegafur Gimeracil Oteracil in Locally Advanced Squamous Cell Carcinoma of the Head and Neck
- A Study of Apatinib for Advanced Hepatocellular Carcinoma Patients After First-line Treatment Failure
- A Study of Apatinib in Recurrent/Metastatic Adenoid Cystic Carcinoma of the Head and Neck
- A Study of Apatinib Mesylate (YN968D1) 1,000mg in Gastric Cancer Patient Failed to Standard Treatment
- A Study of Apatinib Plus Radiotherapy and S-1 for Treatment of Refractory or Metastatic Esophageal Squamous Cell Carcinoma
- A Study of Apatinib Plus Tegafur Gimeracil Oteracil in Recurrent/Metastatic Head and Neck Cancers
- A Study of HIPEC Plus Apatinib and S-1 Conversion Therapy for Gastric Cancer With Positive Exfoliative Cancer Cells
- A Study of Paclitaxel Combined With Apatinib and Adebrelimab in Gastric/Gastroesophageal Junction Adenocarcinoma
- A Study of RC48-ADC in Local Advanced or Metastatic Gastric Cancer With the HER2-Overexpression
- A Study of TACE Combined With Camrelizumab Plus Rivoceranib (Apatinib) in Patients With Incurable Hepatocellular Carcinoma
- A Study to Evaluate Camrelizumab Plus Rivoceranib (Apatinib) Versus Camrelizumab as Adjuvant Therapy in Patients With Hepatocellular Carcinoma (HCC) at High Risk of Recurrence After Curative Resection or Ablation
- A Study to Evaluate the Pharmacokinetics of Apatinib in Subjects With Impaired Renal Function
In development for (25)
- Adenoid cystic carcinoma Phase 2
- Breast cancer Phase 3
- Cancer Phase 1
- Colorectal cancer Phase 2
- Colorectal neoplasm Phase 2
- Differentiated thyroid carcinoma Phase 2
- Esophageal squamous cell carcinoma Phase 2
- Gallbladder carcinoma Phase 2
- Gastric adenocarcinoma Phase 3
- Gastric cancer Phase 3
- Gastric carcinoma Phase 3
- Gastroesophageal junction adenocarcinoma Phase 2
- Head and neck squamous cell carcinoma Phase 2
- Hepatocellular carcinoma Phase 3
- Melanoma Phase 2
- Nasopharyngeal carcinoma Phase 2
- Neoplasm Phase 1
- Neuroblastoma Phase 1
- Non-small cell lung carcinoma Phase 3
- Osteosarcoma Phase 2
Other linked conditions (3)
- Malignant epithelial tumor of ovary
- Meningioma
- Ovarian carcinoma
Targets (1)
- KDR Vascular endothelial growth factor receptor 2 inhibitor