Page last updated: 2024-12-11

akr 501

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

Description

avatrombopag: enhances megakaryocytopoiesis; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9852519
CHEMBL ID2103883
SCHEMBL ID289354
MeSH IDM0527096

Synonyms (59)

Synonym
D10306
avatrombopag (usan/inn)
unii-3h8gsz4sql
akr 501
3h8gsz4sql ,
1-(3-chloro-5-((4-(4-chloro-2-thienyl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl)carbamoyl)-2-pyridyl)piperidine-4-carboxylic acid
as 1670542
570406-98-3
4-piperidinecarboxylic acid, 1-(3-chloro-5-(((4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolyl)amino)carbonyl)-2-pyridinyl)-
e5501
avatrombopag [usan:inn]
ym477
avatrombopag
e 5501
e5501 compound
akr501
ym 477
doptelet
e-5501
akr-501
ym-477
CHEMBL2103883
ym-301477
1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl]carbamoyl}pyridin-2-yl)piperidine-4-carboxylic acid
avatrombopag [who-dd]
1-(3-chloro-5-((4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl)carbamoyl)-2-pyridyl)piperidine-4-carboxylic acid
avatrombopag [inn]
avatrombopag [mi]
avatrombopag [usan]
S6624
SCHEMBL289354
1-[3-chloro-5-[[[4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolyl]amino]carbonyl]-2-pyridinyl]-4-piperidinecarboxylic acid
CS-3397
1-(3-chloro-5-((4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl)carbamoyl)pyridin-2-yl)piperidine-4-carboxylic acid
HY-13463
DTXSID30205667 ,
AKOS027323962
DB11995
FT-0728753
BCP28031
gtpl9953
1-[3-chloro-5-[[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)-1,3-thiazol-2-yl]carbamoyl]pyridin-2-yl]piperidine-4-carboxylic acid
SB16846
AMY40535
e5501;akr-501;ym477
Q27257213
F85065
MS-30955
570406-98-3 (free base)
avatrombopag free base
(1-(3-chloro-5-((4-(4-chloro-2-thienyl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl)carbamoyl)-2-pyridyl)piperidine-4-carboxylic acid)
VXA40698
EN300-18167306
1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)-1,3-thiazol-2-yl]carbamoyl}pyridin-2-yl)piperidine-4-carboxylic acid
b02bx08
avatrombopagum
dtxcid60128158
EX-A6599
akr-501;e5501;ym477

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Outcomes included durable platelet response; need for rescue therapy; reduction in use of concomitant ITP medication; incidence of any or World Health Organization (WHO) grade 2-4 bleeding events, and any adverse events."( Efficacy and Safety of Avatrombopag in Patients with Chronic Immune Thrombocytopenia: A Systematic Literature Review and Network Meta-Analysis.
Jurczak, W; McCrae, KR; Nazir, J; Pochopien, M; Pustułka, I; Smela, B; Tytuła, A; Vredenburg, M; Wilson, K; Wojciechowski, P, 2021
)
0.62
" No statistically significant differences were observed for any adverse events."( Efficacy and Safety of Avatrombopag in Patients with Chronic Immune Thrombocytopenia: A Systematic Literature Review and Network Meta-Analysis.
Jurczak, W; McCrae, KR; Nazir, J; Pochopien, M; Pustułka, I; Smela, B; Tytuła, A; Vredenburg, M; Wilson, K; Wojciechowski, P, 2021
)
0.62
"The aim of the study was to conduct a network meta-analysis to assess the efficacy and incidence of treatment-related adverse events (TRAEs) of eltrombopag, romiplostim, avatrombopag, recombinant human thrombopoietin (rhTPO), and hetrombopag for adult immune thrombocytopenia (ITP)."( Efficacy and Incidence of Treatment-Related Adverse Events of Thrombopoietin Receptor Agonists in Adults with Immune Thrombocytopenia: A Systematic Review and Network Meta-Analysis of Randomized Controlled Study.
Feng, CX; Geng, QC; Lin, X; Liu, Y; Su, J; Zhang, HX, 2023
)
0.91
" The results of meta-analysis showed that in adult patients, patients treated with TPO-RAs had longer duration of platelet response, higher platelet response rate, lower use of rescue therapy, and lower incidence of bleeding events, and similar incidence of adverse events compared with placebo."( Efficacy and safety of thrombopoietin receptor agonists in children and adults with persistent and chronic immune thrombocytopenia: a meta-analysis.
Li, T; Liu, J; Liu, Q; Pu, T; Zhang, A, 2023
)
0.91
"The median treatment time of avatrombopag was 34 days, and no patients stopped treatment due to adverse reactions or drug intolerance."( Efficacy and safety of avatrombopag for thrombocytopenia following allogeneic hematopoietic stem cell transplantation: A real-world data evaluation on 14 cases.
Chen, Y; Fang, P; Li, S; Liu, E; Liu, Y; Xin, H; Xu, Y, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" Following single dosing under fasted and fed conditions, mean peak concentrations occurred at 5 to 8 hours and subsequently declined with a half-life of 16 to 18 hours in Japanese and white subjects."( Pharmacokinetics, Pharmacodynamics, Pharmacogenomics, Safety, and Tolerability of Avatrombopag in Healthy Japanese and White Subjects.
Aluri, J; Ferry, J; Han, D; Nomoto, M; Pastino, G; Rege, B, 2018
)
0.48
"16-fold increase of AUC of avatrombopag, prolonged terminal elimination phase half-life (from 19."( Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs.
Aluri, J; Boyd, P; Chang, MK; Ferry, J; Lai, WG; Nomoto, M; Rege, B; Schuck, E; Siu, YA; Yasuda, S; Zamora, CA, 2018
)
0.48

Compound-Compound Interactions

ExcerptReferenceRelevance
" Here, we report that AKR-501 in combination with TPO has additive effect on megakaryocytopoiesis."( AKR-501 (YM477) in combination with thrombopoietin enhances human megakaryocytopoiesis.
Abe, M; Fukushima-Shintani, M; Hirayama, F; Iwatsuki, Y; Kawasaki, T; Sugasawa, K; Suzuki, K, 2008
)
0.35
" We assessed three drug-drug interactions of avatrombopag as a victim with dual or selective CYP2C9/3A inhibitors and inducers."( Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs.
Aluri, J; Boyd, P; Chang, MK; Ferry, J; Lai, WG; Nomoto, M; Rege, B; Schuck, E; Siu, YA; Yasuda, S; Zamora, CA, 2018
)
0.48

Dosage Studied

ExcerptRelevanceReference
" Following single dosing under fasted and fed conditions, mean peak concentrations occurred at 5 to 8 hours and subsequently declined with a half-life of 16 to 18 hours in Japanese and white subjects."( Pharmacokinetics, Pharmacodynamics, Pharmacogenomics, Safety, and Tolerability of Avatrombopag in Healthy Japanese and White Subjects.
Aluri, J; Ferry, J; Han, D; Nomoto, M; Pastino, G; Rege, B, 2018
)
0.48
" Chemical structures, available dosage forms, recommended dosing, pharmacokinetics, results of toxicity studies in animals, most frequent adverse effects, significant outcomes of the corresponding clinical trials, and their use in specific patient populations are thoroughly described."( New Small Molecule Drugs for Thrombocytopenia: Chemical, Pharmacological, and Therapeutic Use Considerations.
Al-Horani, RA; Clemons Bankston, P, 2019
)
0.51
" Although TPO-RAs are often selected as treatments for chronic ITP, when choosing between the TPO-RAs, clinicians must balance safety profile, dosing restrictions, and method of administration incorporating patient preference."( An updated evaluation of avatrombopag for the treatment of chronic immune thrombocytopenia.
Al-Samkari, H; Song, AB, 2022
)
0.72
"Compared with other TPO-RAs used to treat ITP, avatrombopag offers practical oral dosing with a single pill strength, does not require long-term dietary restrictions, and has no warning for hepatotoxicity."( An updated evaluation of avatrombopag for the treatment of chronic immune thrombocytopenia.
Al-Samkari, H; Song, AB, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (54)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (5.56)29.6817
2010's19 (35.19)24.3611
2020's32 (59.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.62

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 Index16.62 (24.57)
Research Supply Index4.20 (2.92)
Research Growth Index5.64 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.62)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (20.00%)5.53%
Reviews17 (30.91%)6.00%
Case Studies7 (12.73%)4.05%
Observational1 (1.82%)0.25%
Other19 (34.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]