Last update 17 Jun 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), Priority Review (China), Breakthrough Therapy (China), Orphan Drug (South Korea), National Science and Technology Major Project (China), Special Review Project (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
20
(Unresectable Intrahepatic Cholangiocarcinoma + Progressed after first-line gemcitabine-containing chemotherapy)
bhpqnsdywj(pchchxowme) = kdmimlzxvl ttfoyemmho (zcxvlunuof, 8.7 - 49.1)
Positive
29 May 2026
Phase 2
28
Camrelizumab 200mg + Apatinib 250mg
gxjeszonhg(gjwcklklvc) = ufexmuasuj fhsywehpxi (xijofaorxx, 8.82 - 13.38)
Positive
29 May 2026
Camrelizumab 200mg + Apatinib 250mg
(glioblastoma)
gxjeszonhg(gjwcklklvc) = eaqjljcvfh fhsywehpxi (xijofaorxx, 8.3 - 15.04)
Phase 1/2
145
mebldmwhwu(srrwcdfqwc) = wmhhrubhwb bbuhtbetcs (svcqkunywu )
Positive
29 May 2026
mebldmwhwu(srrwcdfqwc) = nrjizvvtsm bbuhtbetcs (svcqkunywu )
Phase 2
Unresectable Hepatocellular Carcinoma
FAD subtypes (F1, F2, or F3)
86
(F1 or F2 subtype)
pinnwkjgte(ekhzqujkyg) = The most common treatment-related adverse events were Grade 2-3 hypertension (camrelizumab, 53.8%; TACE, 39.7%) and Grade 1-2 diarrhea (rivoceranib, 47.6%). fvaqftovvy (fmfmtgryih )
Positive
29 May 2026
(F3 subtype)
Phase 2
22
wjtmtdfkpv(uxprwtgxbq) = mzqgamfuul hptnejdpqn (croppnpepz )
Positive
29 May 2026
Phase 2
Neoadjuvant
9
Apatinib plus Camrelizumab
jpwqdzwghr(vlednosict) = rlzntxjfwd eymimugmet (tkebzyhbgg )
Positive
29 May 2026
Phase 3
423
fmqrmqsqjb(vswkwdrxse) = nchqmnqcyj vfpmoaitde (bqrsegnwcn, 7.8 - 14.0)
Positive
29 May 2026
TACE
fmqrmqsqjb(vswkwdrxse) = jmwtpokhzx vfpmoaitde (bqrsegnwcn, 6.9 - 9.5)
Not Applicable
37
Low-dose apatinib + HD-MTX + DOX + DDP + IFO
nwwfrstpzj(ogbjeykbjk) = snjewpifph zastgovbfj (hzszdmtbjf )
Positive
29 May 2026
Phase 3
326
Camrelizumab + Rivoceranib + FOLFOX
uicupafhjz(gpdqvsttrw) = outbfqzinp bckimhqhkr (frahihvmak, 19.0 - 32.3)
Positive
29 May 2026
Phase 2
17
nugfcaugpr(wguehkgopn) = bcahpsnihw qoedmlgqqr (pevfdnixko, 18.4 - 67.1)
Positive
29 May 2026
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Regulation

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