> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/rivoceranib-77932dd2-2af1-44e3-ba1a-24c963386df3
> Record changed: 2026-10-13

# Rivoceranib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

**Drug name**

Rivoceranib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

**Molecular weight**

397.48

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

**Structure (SMILES)**

N#CC1(c2ccc(NC(=O)c3cccnc3NCc3ccncc3)cc2)CCCC1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

### Other names (16)

- 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

## Identifiers

**CAS registry numbers**

- 811803-05-1

**ChEMBL ID**

CHEMBL3186534

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

**InChIKey**

WPEWQEMJFLWMLV-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3186534)

**PubChem compound IDs**

- 11315474

**FDA ingredient codes (UNII)**

- 5S371K6132

## Regulatory information

### Other regulatory facts

**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

### Drug classification

**Pharmacology name**

rivoceranib

**Type**

Synthetic organic

**Drug name stem**

\-anib

**Approval recorded by Guide to Pharmacology**

Yes

### Mechanisms of action (4)

- **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

### DrugCentral mechanisms (5)

- **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

### Investigated indications (66)

- **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.

### Open Targets indications (139)

- **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.

### Reported adverse events (31)

- **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.

### Trial references (286)

- NCT00633490  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00633490)
- NCT04282278  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04282278)
- NCT04428086  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04428086)
- NCT04569916  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04569916)
- NCT04832204  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04832204)
- NCT00970138  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00970138)
- NCT02409199  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02409199)
- NCT03355612  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03355612)
- NCT03599778  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03599778)
- NCT01176669  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01176669)
- NCT02768415  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02768415)
- NCT02878057  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02878057)
- NCT03086785  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03086785)
- NCT03254654  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03254654)
- NCT03348098  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03348098)
- NCT03394287  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03394287)
- NCT03457467  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03457467)
- NCT03535961  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03535961)
- NCT03580395  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03580395)
- NCT03735082  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03735082)
- NCT03945604  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03945604)
- NCT03982485  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03982485)
- NCT04296370  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04296370)
- NCT04303741  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04303741)
- NCT04335006  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04335006)

And 261 more, listed on the interactive page.

## Chemical properties

**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

## Evidence counts

**Recorded assays**

717

**Active assays**

30

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Pharmacologic actions

- 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](https://trialight.com/data/trial/a-lm-302-combination-with-other-anti-tumor-therapies-phase-f867e7b8-f10d-4281-8491-ff6441459c77.md)
- 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](https://trialight.com/data/condition/adenoid-cystic-carcinoma-6c5702ee-925e-504d-8b2d-477a0008f140.md) Phase 2
- [Biliary tract cancer](https://trialight.com/data/condition/biliary-tract-cancer-6b9535c9-ccaa-5b47-8c46-0d05d39d7c62.md) Phase 2
- [Biliary tract neoplasm](https://trialight.com/data/condition/biliary-tract-neoplasm-5b757066-5940-52f7-aa7d-e5aafdc5b54e.md) Phase 2
- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 3
- [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md) Phase 3
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 2
- [Carcinoma](https://trialight.com/data/condition/carcinoma-575e4c82-5fa5-5455-b1b7-30972eca1a2f.md) Phase 2
- Carcinoma of esophagus Phase 3
- [Cervical cancer](https://trialight.com/data/condition/cervical-cancer-10fb8f6c-5aac-5281-8f06-7238adeec443.md) Phase 2
- Cervical carcinoma Phase 2
- [Cholangiocarcinoma](https://trialight.com/data/condition/cholangiocarcinoma-3777afe4-5189-5eb1-82f8-0c3446cb902f.md) Phase 2
- [Colorectal adenocarcinoma](https://trialight.com/data/condition/colorectal-adenocarcinoma-49107d5a-ece1-5f2b-8783-f2077e298ffa.md) Phase 3
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 3
- [Colorectal neoplasm](https://trialight.com/data/condition/colorectal-neoplasm-31f0a633-3abe-5df4-9d3a-9292c6541f1d.md) Phase 3
- Digestive system cancer Phase 2
- [Esophageal cancer](https://trialight.com/data/condition/esophageal-cancer-a3b5271c-e6d4-537b-8dfd-9391c60e2af2.md) Phase 3
- [Esophageal squamous cell carcinoma](https://trialight.com/data/condition/esophageal-squamous-cell-carcinoma-c10bd9c9-02f9-5805-8008-b021f4604e7a.md) Phase 3
- Exocrine pancreatic carcinoma Phase 2
- [Gallbladder carcinoma](https://trialight.com/data/condition/gallbladder-carcinoma-0f30c5c6-4ee3-58f9-a97d-6499bb1158fb.md) Phase 2
- [Gastric adenocarcinoma](https://trialight.com/data/condition/gastric-adenocarcinoma-6bb74a55-7ba6-53e3-a113-22296a84d6ae.md) Phase 3

### Other linked conditions (1)

- Non-small cell squamous lung carcinoma

### Targets (1)

- [KDR](https://trialight.com/data/target/kdr-4ab08263-0477-533e-ac3f-96e20d343c4b.md) Vascular endothelial growth factor receptor 2 inhibitor

---

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