Last update 07 Jan 2026

Apatinib Mesylate

Overview

Basic Info

Drug Type
Small molecule drug
Synonyms
Apatinib, Rivoceranib, Rivoceranib mesilate
+ [5]
Target
Action
antagonists
Mechanism
VEGFR2 antagonists(Vascular endothelial growth factor receptor 2 antagonists)
Originator Organization
Drug Highest PhaseApproved
RegulationOrphan Drug (United States), Orphan Drug (European Union), Breakthrough Therapy (China), Special Review Project (China), Orphan Drug (South Korea), National Science and Technology Major Project (China), Priority Review (China)
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Structure/Sequence

Molecular FormulaC25H27N5O4S
InChIKeyFYJROXRIVQPKRY-UHFFFAOYSA-N
CAS Registry1218779-75-9

External Link

KEGGWikiATCDrug Bank
-Apatinib Mesylate

R&D Status

Approved
10 top approved records.
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IndicationCountry/LocationOrganizationDate
Germline BRCA-mutated, HER2-negative metastatic breast cancer
China
01 Dec 2024
Hepatocellular Carcinoma
China
07 Jan 2021
Gastroesophageal junction adenocarcinoma
China
17 Oct 2014
stomach adenocarcinoma
China
17 Oct 2014
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
Metastatic hepatocellular carcinomaNDA/BLA
United States
21 Oct 2024
Unresectable Hepatocellular CarcinomaNDA/BLA
United States
17 May 2023
Stomach CancerNDA/BLA
China
09 Aug 2011
Advanced Gastroesophageal Junction AdenocarcinomaPhase 3
China
21 Sep 2020
Advanced Lung Non-Small Cell CarcinomaPhase 3
China
16 Sep 2020
Advanced Triple-Negative Breast CarcinomaPhase 3
China
06 Jul 2020
Breast CancerPhase 3
China
03 Jul 2020
Metastatic breast cancerPhase 3
China
03 Jul 2020
PD-L1 positive Lung CancerPhase 3-15 Jun 2020
PD-L1 positive Non-Small Cell Lung CancerPhase 3-15 Jun 2020
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 2
Triple Negative Breast Cancer
Neoadjuvant
HER2 Negative | PR Negative | ER Negative
35
Camrelizumab+apatinib+chemotherapy
umpuofpoqx(sabyxtubez) = Elevated levels of alanine aminotransferase (38.2%) gxhmvxdkzl (crfytujgvp )
Positive
11 Dec 2025
Not Applicable
1,586
bojhzrmbzx(xhenbsdcll): HR = 0.42 (95.0% CI, 0.36 - 0.49), P-Value = < 0.00001
Positive
05 Dec 2025
Phase 3
543
Camrelizumab 200 mg + Rivoceranib 250 mg
tlcshkfsvd(tcxylnbmko) = prtjdrjlvf escxbxpwuj (kdkzuimzpv, 20.6 - 27.2)
Positive
01 Dec 2025
tlcshkfsvd(tcxylnbmko) = axbuueeykc escxbxpwuj (kdkzuimzpv, 13.2 - 18.5)
Phase 3
Germline BRCA-mutated, HER2-negative metastatic breast cancer
HER2 Negative | BRCA1 Mutation (Germline) | BRCA2 Mutation (Germline)
203
ultlgyykcv(ybxzsforaz) = pwatnuscjr cyzobrksvn (lmssoejvbe, 8.4 - 13.1)
Positive
01 Dec 2025
ultlgyykcv(ybxzsforaz) = mtezgehdej cyzobrksvn (lmssoejvbe, 4.2 - 7.6)
Phase 3
Ovarian Cancer
First line
674
zrqfjmqtny(xgsnshourz) = mwremwvxqe rqkzfpltvf (rxnflsgqyb )
Positive
25 Nov 2025
zrqfjmqtny(xgsnshourz) = qxcngdioof rqkzfpltvf (rxnflsgqyb )
Phase 2/3
Hepatocellular Carcinoma
Neoadjuvant | Adjuvant
294
Perioperative+ camrelizumab + rivoceranib
ajjnrstkux(jzqzfiivgh) = bqeuvbordp kqayxjbmwn (fjjojtfnfp, 23.2 - NE)
Positive
01 Nov 2025
surgery alone
ajjnrstkux(jzqzfiivgh) = luwogwnbmj kqayxjbmwn (fjjojtfnfp, 14·9 - NE)
Phase 2
40
ovcrkqjtgv(qkqjyfleqe) = qlrrmmpezk ywgniazusn (kcqgggbret )
Positive
17 Oct 2025
Phase 2
Sarcoma
VEGFR2 604A>G | CSF1-high
60
(VEGFR2 604A>G SNP)
vzfaiysvbm(ofjxpmcmkw) = obeoovywod bvbbywjlqu (nzhcrtqkbq )
Positive
17 Oct 2025
(VEGFR2 604A>G SNP negative)
vzfaiysvbm(ofjxpmcmkw) = vxfvclkssw bvbbywjlqu (nzhcrtqkbq )
Phase 2
25
mscrrbzdlv(esarslyzoa) = thzdnlkyfj gppsosurmk (jciukbpwjg )
Positive
17 Oct 2025
Phase 2
7
gnikznpkge(orapxdceva) = gxkskuhiwr onrcmszdra (rqgcmeejqr )
Positive
17 Oct 2025
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Core Patent

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Clinical Trial

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Approval

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Regulation

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