Page last updated: 2024-11-13

vt-464

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

Description

VT-464: a CYP17A1 inhibitor with antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID78357816
CHEMBL ID3264610
SCHEMBL ID23299702
MeSH IDM000610159

Synonyms (31)

Synonym
CHEMBL3264610
CS-3139
seviteronel
HY-15996
seviteronel [who-dd]
8S5OIN36X4 ,
1610537-15-9
seviteronel [inn]
1h-1,2,3-triazole-5-methanol, .alpha.-(6,7-bis(difluoromethoxy)-2-naphthalenyl)-.alpha.-(1-methylethyl)-, (.alpha.s)-
(1s)-1-(6,7-bis(difluoromethoxy)naphthalen-2-yl)-2-methyl-1-(1h-1,2,3-triazole-4-yl)propan-1-ol
vt-464
unii-8s5oin36x4
1h-1,2,3-triazole-5-methanol, alpha-(6,7-bis(difluoromethoxy)-2-naphthalenyl)-alpha-(1-methylethyl)-, (alphas)-
AKOS030526607
NCGC00390672-01
DB12275
(1s)-1-[6,7-bis(difluoromethoxy)naphthalen-2-yl]-2-methyl-1-(1h-1,2,3-triazol-4-yl)propan-1-ol
'(1s)-1-[6,7-bis(difluoromethoxy)naphthalen-2-yl]-2-methyl-1-(2h-1,2,3-triazol-4-yl)propan-1-ol'
Q21098941
SB17087
(1s)-1-[6,7-bis(difluoromethoxy)naphthalen-2-yl]-2-methyl-1-(2h-triazol-4-yl)propan-1-ol
SCHEMBL23299702
MS-26762
nsc-783294
nsc783294
nsc-788846
nsc788846
EX-A5986
DTXSID401025651
zbrajoqfsnyjmf-sfhvurjksa-n
1h-1,2,3-triazole-5-methanol, alpha-[6,7-bis(difluoromethoxy)-2-naphthalenyl]-alpha-(1-methylethyl)-, (alphas)-

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
" The disposition of seviteronel following oral administration is well described by this population PK model and can be used for accurate simulations for future studies with body weight and sex affecting clearance, but not to a clinically-meaningful degree requiring a change in the current dosing scheme."( A population pharmacokinetic analysis of the oral CYP17 lyase and androgen receptor inhibitor seviteronel in patients with advanced/metastatic castration-resistant prostate cancer or breast cancer.
Baskin-Bey, E; Brown, VV; Eisner, JR; Figg, WD; Kindrick, JD; Madan, R; Peer, CJ; Schmidt, KT, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (11)

Assay IDTitleYearJournalArticle
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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
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.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1648488Binding affinity to C-terminal 6-His-tagged human CYP17A1 expressed in Escherichia coli assessed as induction of type II binding spectral changes at 50 uM using 1 uM CYP17A1 by spectroscopy2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Multistep Binding of the Non-Steroidal Inhibitors Orteronel and Seviteronel to Human Cytochrome P450 17A1 and Relevance to Inhibition of Enzyme Activity.
AID1648489Binding affinity to C-terminal 6-His-tagged human CYP17A1 expressed in Escherichia coli assessed as induction of spectral changes by measuring rate constant of first reaction at 50 uM using 1 uM CYP17A1 by spectroscopy2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Multistep Binding of the Non-Steroidal Inhibitors Orteronel and Seviteronel to Human Cytochrome P450 17A1 and Relevance to Inhibition of Enzyme Activity.
AID1142266Inhibition of CYP17 in gonadally-intact hamster assessed as progesterone level in serum at 50 mg/kg, po after 2 hrs by LC/MS/MS analysis (Rvb = 1.02 +/- 0.05 ng/mL)2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors.
AID1648490Binding affinity to C-terminal 6-His-tagged human CYP17A1 expressed in Escherichia coli assessed as induction of spectral changes by measuring rate constant of second reaction at 50 uM using 1 uM CYP17A1 by spectroscopy2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Multistep Binding of the Non-Steroidal Inhibitors Orteronel and Seviteronel to Human Cytochrome P450 17A1 and Relevance to Inhibition of Enzyme Activity.
AID1142265Inhibition of CYP17 in gonadally-intact hamster assessed as testosterone level in serum at 50 mg/kg, po after 2 hrs by LC/MS/MS analysis (Rvb = 1.98 +/- 0.057 ng/mL)2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (50.00)24.3611
2020's7 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (7.14%)5.53%
Reviews2 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (78.57%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]