NAV

Proxalutamide

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
Proxalutamide
DrugBank Accession Number
DB16065
Background

Proxalutamide is under investigation in clinical trial NCT03899467 (The Safety and Tolerability of Proxalutamide (GT0918) in Subjects With Metastatic Castrate Resistant Prostate Cancer).

Type
Small Molecule
Groups
Investigational
Structure
3D
Similar Structures
Weight
Average: 517.5
Monoisotopic: 517.119558698
Chemical Formula
C24H19F4N5O2S
Synonyms
  • Proxalutamide
External IDs
  • GT-0918

Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

Proxalutamide is an antagonist at the androgen receptor which leads to inhibition of androgen-induced receptor activation and results in formation of inactive complexes that are not able to translocate to the nucleus. It also induces androgen receptor downregulation, furthering adrogen-induced receptor activation. This drug is being investigated for its potential antineoplastic activity and is being investigated specifically against prostate cancer and COVID-19.

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
QX6O64GP40
CAS number
1398046-21-3
InChI Key
KCBJGVDOSBKVKP-UHFFFAOYSA-N
InChI
InChI=1S/C24H19F4N5O2S/c1-23(2)21(34)32(17-9-6-14(12-29)19(20(17)25)24(26,27)28)22(36)33(23)16-8-7-15(31-13-16)4-3-5-18-30-10-11-35-18/h6-11,13H,3-5H2,1-2H3
IUPAC Name
4-(4,4-dimethyl-3-{6-[3-(1,3-oxazol-2-yl)propyl]pyridin-3-yl}-5-oxo-2-sulfanylideneimidazolidin-1-yl)-3-fluoro-2-(trifluoromethyl)benzonitrile
SMILES
CC1(C)N(C(=S)N(C1=O)C1=C(F)C(=C(C=C1)C#N)C(F)(F)F)C1=CN=C(CCCC2=NC=CO2)C=C1

References

General References
  1. Dellis AE, Papatsoris AG: Perspectives on the current and emerging chemical androgen receptor antagonists for the treatment of prostate cancer. Expert Opin Pharmacother. 2019 Feb;20(2):163-172. doi: 10.1080/14656566.2018.1548611. Epub 2018 Nov 21. [Article]
ChemSpider
52084193
Wikipedia
Proxalutamide

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentCoronavirus Disease 2019 (COVID‑19)1
3CompletedTreatmentCoronavirus Disease 2019 (COVID‑19) / Safety and Efficacy1
3CompletedTreatmentCoronavirus Disease 2019 (COVID‑19) / Severe Acute Respiratory Syndrome (SARS)1
3RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19)1
3WithdrawnTreatmentCoronavirus (SARS-CoV) / Coronavirus Disease 2019 (COVID‑19)1
3WithdrawnTreatmentCoronavirus Disease 2019 (COVID‑19) / Severe Acute Respiratory Syndrome (SARS)1
2RecruitingTreatmentMetastatic Castration-Resistant Prostate Cancer (mCRPC)1
2RecruitingTreatmentNeoadjuvant Therapy \High Risk Prostate Cancer1
1CompletedTreatmentMetastatic Breast Cancer1
1CompletedTreatmentMetastatic Castration-Resistant Prostate Cancer (mCRPC)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0379 mg/mLALOGPS
logP4.65ALOGPS
logP4.53Chemaxon
logS-4.1ALOGPS
pKa (Strongest Basic)4.73Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area86.26 Å2Chemaxon
Rotatable Bond Count7Chemaxon
Refractivity126 m3·mol-1Chemaxon
Polarizability48.98 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created at December 15, 2020 18:03 / Updated at January 20, 2021 07:45