> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/rivoceranib-mesylate-e3d23ea8-6bde-4278-b83d-13515b955293
> Record changed: 2026-11-04

# Rivoceranib mesylate

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

**Drug name**

Rivoceranib mesylate

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

**Molecular weight**

493.59

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

**Structure (SMILES)**

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

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

### Brand names (2)

- aitan
- Aitan

### Other names (15)

- 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

## Identifiers

**CAS registry numbers**

- 1218779-75-9

**ChEMBL ID**

CHEMBL3545414

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

**InChIKey**

FYJROXRIVQPKRY-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545414)

**PubChem compound IDs**

- 45139106

**FDA ingredient codes (UNII)**

- TK02X14ASJ

## Regulatory information

### Other regulatory facts

**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

## Pharmacology

### Drug classification

**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

### Investigated indications (22)

- **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

### Open Targets indications (35)

- **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.

### Reported adverse events (8)

- **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

### Trial references (61)

- NCT01497704  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01497704)
- NCT01726101  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01726101)
- NCT02711969  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02711969)
- NCT03219593  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03219593)
- NCT04006821  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04006821)
- NCT04089657  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04089657)
- NCT04195828  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04195828)
- NCT04338438  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04338438)
- NCT04342910  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04342910)
- NCT04345783  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04345783)
- NCT04714190  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04714190)
- NCT05025033  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05025033)
- NCT05223088  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05223088)
- NCT05524974  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05524974)
- NCT02772029  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02772029)
- NCT04523662  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04523662)
- NCT04850040  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04850040)
- NCT04930315  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04930315)
- NCT05320692  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05320692)
- NCT05613478  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05613478)
- NCT02775370  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02775370)
- NCT02836171  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02836171)
- NCT02836821  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02836821)
- NCT04322552  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04322552)
- NCT04457180  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04457180)

And 36 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

**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

## Evidence counts

**Recorded assays**

12

**Active assays**

1

### Active assay types

- Confirmatory

## Pharmacologic actions

- Antineoplastic Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000970.html)
- Protein Kinase Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D047428.html)

## 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](https://trialight.com/data/trial/a-study-to-evaluate-camrelizumab-plus-rivoceranib-apatinib-52d0f19a-07cc-47b7-aaaf-09d5cf0638ab.md)
- A Study to Evaluate the Pharmacokinetics of Apatinib in Subjects With Impaired Renal Function

### In development for (25)

- [Adenoid cystic carcinoma](https://trialight.com/data/condition/adenoid-cystic-carcinoma-6c5702ee-925e-504d-8b2d-477a0008f140.md) Phase 2
- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 3
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 1
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 2
- [Colorectal neoplasm](https://trialight.com/data/condition/colorectal-neoplasm-31f0a633-3abe-5df4-9d3a-9292c6541f1d.md) Phase 2
- [Differentiated thyroid carcinoma](https://trialight.com/data/condition/differentiated-thyroid-carcinoma-d7c5bae1-a4cb-5587-998c-99d7ccc3ba9a.md) Phase 2
- [Esophageal squamous cell carcinoma](https://trialight.com/data/condition/esophageal-squamous-cell-carcinoma-c10bd9c9-02f9-5805-8008-b021f4604e7a.md) 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
- [Gastric cancer](https://trialight.com/data/condition/gastric-cancer-3c1e2785-2672-5b3e-afce-9335f684c159.md) Phase 3
- Gastric carcinoma Phase 3
- [Gastroesophageal junction adenocarcinoma](https://trialight.com/data/condition/gastroesophageal-junction-adenocarcinoma-de7e280e-cbd1-5266-a5dd-dda00261a706.md) Phase 2
- [Head and neck squamous cell carcinoma](https://trialight.com/data/condition/head-and-neck-squamous-cell-carcinoma-cbc3ae58-4a6c-52e4-a41b-274051db19fa.md) Phase 2
- [Hepatocellular carcinoma](https://trialight.com/data/condition/hepatocellular-carcinoma-fc1014ac-5a3c-551d-98ea-95306009e299.md) Phase 3
- [Melanoma](https://trialight.com/data/condition/melanoma-457e9de6-dcd9-56fb-be48-0290fb4386ef.md) Phase 2
- [Nasopharyngeal carcinoma](https://trialight.com/data/condition/nasopharyngeal-carcinoma-9ead4a97-f794-5dda-b62e-20f8ca202f89.md) Phase 2
- [Neoplasm](https://trialight.com/data/condition/neoplasm-2a973797-359b-5982-907e-98f9b7c1a284.md) Phase 1
- Neuroblastoma Phase 1
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 3
- [Osteosarcoma](https://trialight.com/data/condition/osteosarcoma-d6ad580f-c521-585b-9a22-26006b6bff2b.md) Phase 2

### Other linked conditions (3)

- Malignant epithelial tumor of ovary
- [Meningioma](https://trialight.com/data/condition/meningioma-5ed57dc9-a477-5890-89ce-dc398e272670.md)
- [Ovarian carcinoma](https://trialight.com/data/condition/ovarian-carcinoma-e5ec8fdc-01ec-5cd9-9507-107d23d3a30b.md)

### 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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