Page last updated: 2024-11-13

hmpl-013

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

HMPL-013: a VEGF receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44480399
CHEMBL ID4303214
SCHEMBL ID947183
MeSH IDM000598336

Synonyms (45)

Synonym
S5667
6-((6,7-dimethoxyquinazolin-4-yl)oxy)-n,2-dimethylbenzofuran-3-carboxamide
hmpl 013
BALLNEJQLSTPIO-UHFFFAOYSA-N
6-(6,7-dimethoxyquinazolin-4-yloxy)-n,2-dimethylbenzofuran-3-carboxamide
SCHEMBL947183
hmpl013
fruquintinib [inn]
elunate
gtpl9428
fruquintinib [usan:who-dd]
unii-49dxg3m5zw
fruquintinib [who-dd]
3-benzofurancarboxamide, 6-((6,7-dimethoxy-4-quinazolinyl)oxy)-n,2-dimethyl-
fruquintinib ,
who 10348
49dxg3m5zw ,
1194506-26-7
6-(6,7-dimethoxyquinazolin-4-yl)oxy-n,2-dimethyl-1-benzofuran-3-carboxamide
hmpl-013
fruquintinib [usan]
HY-19912
CS-5558
AKOS026750586
6-[(6,7-dimethoxyquinazolin-4-yl)oxy]-n,2-dimethyl-1-benzofuran-3-carboxamide
AS-73141
fruquintinib (hmpl-013)
DB11679
BCP15692
hmpl-013;hmpl013;hmpl 013
fruquintinib; hmpl-013
EX-A2262
6-[(6,7-dimethoxy-4-quinazolinyl)oxy]-n,2-dimethyl-3-benzofurancarboxamide
SB17123
CCG-268573
CHEMBL4303214
NCGC00481603-01
Q27259271
nsc-829498
nsc829498
C71641
B2693-470819
A898991
nsc801000
nsc-801000

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Adverse events were assessed using National Cancer Institute Common Terminology Criteria for Adverse Events v4."( A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors.
Cao, J; Chen, Z; Fan, S; Li, J; Li, K; Peng, W; Su, W; Zhang, J, 2016
)
0.43
" The most common grade 3/4 adverse events were hand-foot skin reaction, hypertension, and thrombocytopenia."( A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors.
Cao, J; Chen, Z; Fan, S; Li, J; Li, K; Peng, W; Su, W; Zhang, J, 2016
)
0.43
" The most common grade 3-4 adverse events were hypertension and hand-foot skin reaction."( Safety and efficacy of fruquintinib in patients with previously treated metastatic colorectal cancer: a phase Ib study and a randomized double-blind phase II study.
Bai, Y; Cao, J; Fan, S; Hua, Y; Li, J; Liu, T; Pan, H; Shen, L; Su, W; Wang, L; Xu, J; Xu, RH; Zhang, D, 2017
)
0.46
" However, its safety profile, including adverse events of special interest (AESIs) and treatment-emergent adverse events (TEAEs) by age, sex, and body mass index (BMI), is not well known."( Safety Profile and Adverse Events of Special Interest for Fruquintinib in Chinese Patients with Previously Treated Metastatic Colorectal Cancer: Analysis of the Phase 3 FRESCO Trial.
Bai, Y; Cao, P; Chen, D; Chen, H; Chen, Z; Cheng, Y; Deng, Y; Fan, S; Guo, W; Guo, X; Han, R; Li, J; Li, W; Liu, T; Ma, D; Pan, H; Qin, S; Shen, L; Shu, Y; Sun, S; Wang, H; Wang, N; Wang, S; Wu, C; Xu, J; Xu, N; Xu, R; Yang, L; Yu, Z; Yuan, Y; Zhang, B; Zhong, H; Zhou, J, 2020
)
0.56
" The FRESCO-2 study is being conducted globally to determine how safe and effective fruquintinib is at treating patients with metastatic colorectal cancer that has grown or spread following other forms of treatment, such as chemotherapy."( FRESCO-2: a global Phase III study investigating the efficacy and safety of fruquintinib in metastatic colorectal cancer.
Chien, C; Dasari, A; Eng, C; Kania, M; Schelman, W; Sobrero, A; Tabernero, J; Yang, Z; Yao, J; Yoshino, T, 2021
)
0.62
" The main adverse events (AEs) included reactive cutaneous capillary endothelial proliferation (RCCEP) (81."( Efficacy and safety of regorafenib or fruquintinib plus camrelizumab in patients with microsatellite stable and/or proficient mismatch repair metastatic colorectal cancer: an observational pilot study.
Jiang, FE; Liu, AN; Yu, CY; Zhang, HJ, 2021
)
0.62
" The primary outcome was time-to-treatment failure (TTF), and secondary outcomes were overall survival (OS) and adverse events."( Efficacy and Safety Comparison of Regorafenib and Fruquintinib in Metastatic Colorectal Cancer-An Observational Cohort Study in the Real World.
Cao, Y; Chen, M; Li, J; Lu, M; Peng, Z; Qi, C; Shen, L; Wang, X; Wang, Z; Zhang, J; Zhang, Q, 2022
)
0.72
" The incidences of most adverse events were similar between the two groups, while any grade of hand-foot skin reaction and hyperbilirubinemia were more frequently observed in the regorafenib group and ≥grade 3 hypertension was more common in the fruquintinib group."( Efficacy and Safety Comparison of Regorafenib and Fruquintinib in Metastatic Colorectal Cancer-An Observational Cohort Study in the Real World.
Cao, Y; Chen, M; Li, J; Lu, M; Peng, Z; Qi, C; Shen, L; Wang, X; Wang, Z; Zhang, J; Zhang, Q, 2022
)
0.72
" The DCR, progression-free survival (PFS), and adverse reactions of the drug were recorded and reviewed."( Efficacy and safety of fruquintinib as third- or further-line therapy for patients with advanced bone and soft tissue sarcoma: a multicenter retrospective study.
Ding, X; Hu, H; Li, Q; Liang, J; Liu, Y; Zhang, Y; Zhou, Y, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" It shows moderate oral bioavailability of 42-53 % and Tmax < 4 h in mouse, rat, dog and monkey, with exposure-dose linearity proved in rats and dogs."( Preclinical pharmacokinetics and disposition of a novel selective VEGFR inhibitor fruquintinib (HMPL-013) and the prediction of its human pharmacokinetics.
Gu, Y; Guo, L; Li, K; Ren, H; Sai, Y; Su, W; Wang, J; Zhang, L; Zhang, W, 2014
)
0.62
" Pharmacokinetic parameters were measured after a single dose and in multiple dosing."( A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors.
Cao, J; Chen, Z; Fan, S; Li, J; Li, K; Peng, W; Su, W; Zhang, J, 2016
)
0.43
" PK analysis showed good and rapid absorption followed by slow terminal elimination with a mean half-life of approximately 42 h which was consistent across all dose groups."( A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors.
Cao, J; Chen, Z; Fan, S; Li, J; Li, K; Peng, W; Su, W; Zhang, J, 2016
)
0.43
" The objective of the study was to investigate the tolerability and effect of high-fat food on the pharmacokinetic profile of a fruquintinib capsule in healthy Chinese subjects."( Effects of a High-fat Meal on the Pharmacokinetics of the VEGFR Inhibitor Fruquintinib: A Randomized Phase I Study in Healthy Subjects.
Chen, Q; Fan, S; Jia, J; Li, K; Li, T; Liu, Y; Qian, H; Sai, Y; Su, W; Wang, W; Yu, C, 2019
)
0.51
" Blood samples for pharmacokinetic analysis were collected at the designated time points."( Effects of a High-fat Meal on the Pharmacokinetics of the VEGFR Inhibitor Fruquintinib: A Randomized Phase I Study in Healthy Subjects.
Chen, Q; Fan, S; Jia, J; Li, K; Li, T; Liu, Y; Qian, H; Sai, Y; Su, W; Wang, W; Yu, C, 2019
)
0.51
" The analytical method had been validated and applied to a pharmacokinetic study of fruquintinib in rat."( Validated UPLC-MS/MS method for quantification of fruquintinib in rat plasma and its application to pharmacokinetic study.
Guo, J; Luo, SB; Mei, YB; Qiu, XJ; Xie, SL; Ye, LY; Zhang, Q, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" It shows moderate oral bioavailability of 42-53 % and Tmax < 4 h in mouse, rat, dog and monkey, with exposure-dose linearity proved in rats and dogs."( Preclinical pharmacokinetics and disposition of a novel selective VEGFR inhibitor fruquintinib (HMPL-013) and the prediction of its human pharmacokinetics.
Gu, Y; Guo, L; Li, K; Ren, H; Sai, Y; Su, W; Wang, J; Zhang, L; Zhang, W, 2014
)
0.62
"The overall bioavailability of the evaluated formulation of fruquintinib was not affected by the consumption of a high-fat, high-calorie meal prior to dosing."( Effects of a High-fat Meal on the Pharmacokinetics of the VEGFR Inhibitor Fruquintinib: A Randomized Phase I Study in Healthy Subjects.
Chen, Q; Fan, S; Jia, J; Li, K; Li, T; Liu, Y; Qian, H; Sai, Y; Su, W; Wang, W; Yu, C, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" It would require high potency (low effective drug concentrations) and sufficient drug exposures at tolerated doses so that the drug concentration can be maintained above effective drug concentration for target inhibition within the dosing period."( Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy.
Cai, H; Cui, Y; Gu, Y; Guo, M; Hong, M; Liang, J; Long, J; Ni, L; Qing, W; Ren, Y; Sai, Y; Su, W; Sun, J; Sun, Q; Yang, H; Yang, Z; Yin, F; Zhang, M; Zhang, W; Zhang, Z; Zhou, F; Zhou, J, 2014
)
0.4
" Steady-state was achieved after 14 days of QD dosing with systemic exposure four-fold higher than that after a single dose."( Phase 1/1b open-label, dose-escalation study of fruquintinib in patients with advanced solid tumors in the United States.
Chien, C; Gonzalez, M; Kania, M; Schelman, W; Ukrainskyj, S; Wang-Gillam, A; Yang, Z; Yeckes-Rodin, H, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1345548Human fms related tyrosine kinase 1 (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family)2014Cancer biology & therapy, , Volume: 15, Issue:12
Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy.
AID1345520Human fms related tyrosine kinase 4 (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family)2014Cancer biology & therapy, , Volume: 15, Issue:12
Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy.
AID1345506Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family)2014Cancer biology & therapy, , Volume: 15, Issue:12
Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's17 (39.53)24.3611
2020's26 (60.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.26

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.26 (24.57)
Research Supply Index4.06 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials13 (29.55%)5.53%
Reviews8 (18.18%)6.00%
Case Studies2 (4.55%)4.05%
Observational2 (4.55%)0.25%
Other19 (43.18%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]