Identification
- Summary
Darolutamide is an androgen receptor antagonist used for castration-resistant, non-metastatic prostate cancer and metastatic hormone-sensitive prostate cancer.
- Brand Names
- Nubeqa
- Generic Name
- Darolutamide
- DrugBank Accession Number
- DB12941
- Background
Darolutamide is a nonsteroidal androgen receptor antagonist for the treatment of castrate-resistant, non-metastatic prostate cancer (nmCRPC). This condition occurs in the majority of patients with advanced prostate cancer who have been treated with androgen receptor antagonists.4 Though prior treatment for prostate cancer has been successful for these patients, the cancer eventually progresses to become resistant to existing therapies. This warrants further treatment.
The goal of treatment with darolutamide is to delay the progression of prostate cancer to metastatic disease, increasing quality of life and life expectancy for those with advanced prostate cancer.2,4 Darolutamide was developed by Bayer HealthCare Pharmaceuticals Inc. and approved by the FDA on July 30th, 2019.8
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Darolutamide (DB12941)
- Weight
- Average: 398.85
Monoisotopic: 398.1258016 - Chemical Formula
- C19H19ClN6O2
- Synonyms
- Darolutamide
- External IDs
- BAY 1841788
- BAY-1841788
- BAY1841788
- ODM-201
Pharmacology
- Indication
Darolutamide is indicated for the treatment of adults with non-metastatic castration-resistant prostate cancer (nmCRPC) and metastatic hormone-sensitive prostate cancer (mHSPC) in combination with docetaxel.10
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Metastatic hormone sensitive prostate cancer Regimen in combination with: Docetaxel (DB01248) •••••••••••• ••••• •••••• Treatment of Non-mestatatic castrate-resistant prostate cancer •••••••••••• ••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Darolutamide, through its downstream effects on cancer cell growth, treats castrate-resistant prostate cancer. It inhibits cancer cell growth and markedly lowers prostate specific antigen (PSA) levels through potent androgen receptor antagonism.3,4,6
- Mechanism of action
The actions of androgens on androgen receptors (AR) potentiate the growth and survival of prostate cancer cells.5 Darolutamide competitively inhibits androgens from binding to their receptors, inhibiting AR nuclear translocation, as well as AR-mediated transcription. The end result of these processes is a decrease in prostate cancer cell proliferation and tumor size.6 Its main metabolite, keto-darolutamide, shows similar pharmacological activity to the parent drug, darolutamide.4,6 Darolutamide has been found to bind more tightly to the AR receptor than apalutamide and enzalutamide, which are other androgen receptor antagonists.3,5
Darolutamide can act as a progesterone receptor (PR) antagonist in the laboratory setting with approximately 1% activity when compared to its actions at the androgen receptor. The clinical relevance is not known at this time.6
Target Actions Organism AAndrogen receptor antagonistHumans UProgesterone receptor antagonistHumans - Absorption
Darolutamide is absorbed in the gastrointestinal tract.6 In the fasted state, peak concentrations are reached within 3-5 hours, and within 3-8 hours in the fed state. Median Tmax is between 3-6 hours.2The average darolutamide steady-state peak plasma concentration after a 600 mg twice daily dose is approximately 4.79 mg/L. The Cmax is attained approximately 4 hours after administration of a single 600 mg oral dose. The AUC 0-12h is approximately 52.82 h•μg/mL.6
Effects of food
The absolute bioavailability of darolutamide is approximately 30% after fasting and taking a single 300 mg dose. Steady-state concentrations are attained between 2 and 5 days after repeated administration with food. The bioavailability of darolutamide increases by 2.0 to 2.5 times when it is given with food.4,6,9
- Volume of distribution
After intravenous administration, the apparent volume of distribution of darolutamide is about 119L.6
- Protein binding
The plasma protein binding for darolutamide is 92% and 99.8% for keto-darolutamide, the active metabolite. They are mainly bound to albumin.6
- Metabolism
Darolutamide is mainly metabolized by the CYP3A4 hepatic microsomal enzyme1 in addition to UGT1A9 and UGT1A1. The main active metabolite keto-darolutamide in found in the plasma at 2 times the concentration of darolutamide.6
Hover over products below to view reaction partners
- Route of elimination
In a pharmacokinetic study, a radiolabeled dose of darolutamide in an oral solution showed that 63.4% of darolutamide-related material was excreted in the urine (7% of which was unchanged drug) and 32.4% in the feces (with 30% unchanged drug).6
- Half-life
The half-life of darolutamide and its active metabolite, keto-darolutamide is about 20 hours.6 A phase 1 study determined a terminal half life ranging between 10-15 hours.2
- Clearance
The clearance of darolutamide after an intravenous dose is 116 mL/min (39.7%).6
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
LD50 information for darolutamide is not readily available in the literature.
To this date, there is no known antidote in existence for an overdose with darolutamide. The highest dose clinically documented was a twice daily dose of 900 mg, totalling 1800 mg. Dose-limiting toxicities have not been observed with this drug. In patients with healthy kidney and liver function, a high dose of darolutamide will likely not lead to systemic toxicity.6 If a high dose (higher than recommended on labeling) is ingested in a patient with renal or hepatic impairment, and toxic symptoms occur, pause treatment with darolutamide and offer supportive treatment until symptoms resolve.6
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Darolutamide can be increased when it is combined with Abametapir. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Darolutamide. Abrocitinib The serum concentration of Darolutamide can be increased when it is combined with Abrocitinib. Adagrasib The serum concentration of Darolutamide can be increased when it is combined with Adagrasib. Adenine The metabolism of Darolutamide can be decreased when combined with Adenine. - Food Interactions
- Avoid St. John's Wort. This herb induces CYP3A and P glycoprotein and may reduce the serum concentration of darolutamide.
- Take with food. This increases the bioavailability of darolutamide.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Nubeqa
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nubeqa Tablet, film coated 300 mg Oral Bayer Ag 2020-12-16 Not applicable EU 
Nubeqa Tablet, film coated 300 mg/1 Oral Bayer HealthCare Pharmaceuticals Inc. 2019-07-31 Not applicable US 
Nubeqa Tablet, film coated 300 mg Oral Bayer Ag 2020-12-16 Not applicable EU Nubeqa Tablet 300 mg Oral Bayer 2020-03-24 Not applicable Canada 
Categories
- ATC Codes
- L02BB06 — Darolutamide
- Drug Categories
- Androgen Receptor Inhibitors
- Antiandrogens
- Antiandrogens, non-steroidal
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- BCRP/ABCG2 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Endocrine Therapy
- Hormone Antagonists and Related Agents
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- P-glycoprotein substrates
- UGT1A1 Substrates
- UGT1A9 Substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpyrazoles. These are compounds containing a phenylpyrazole skeleton, which consists of a pyrazole bound to a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Azoles
- Sub Class
- Pyrazoles
- Direct Parent
- Phenylpyrazoles
- Alternative Parents
- Pyrazole-5-carboxamides / Benzonitriles / 2-heteroaryl carboxamides / Chlorobenzenes / Aryl chlorides / Heteroaromatic compounds / Secondary carboxylic acid amides / Secondary alcohols / Nitriles / Azacyclic compounds show 4 more
- Substituents
- 2-heteroaryl carboxamide / Alcohol / Aromatic alcohol / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Benzonitrile / Carbonitrile show 20 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- X05U0N2RCO
- CAS number
- 1297538-32-9
- InChI Key
- BLIJXOOIHRSQRB-PXYINDEMSA-N
- InChI
- InChI=1S/C19H19ClN6O2/c1-11(22-19(28)18-8-17(12(2)27)23-24-18)10-26-6-5-16(25-26)13-3-4-14(9-21)15(20)7-13/h3-8,11-12,27H,10H2,1-2H3,(H,22,28)(H,23,24)/t11-,12?/m0/s1
- IUPAC Name
- N-[(2S)-1-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]propan-2-yl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
- SMILES
- C[C@@H](CN1C=CC(=N1)C1=CC=C(C#N)C(Cl)=C1)NC(=O)C1=NNC(=C1)C(C)O
References
- Synthesis Reference
Pan T, Xia C, Jiang H, Zhang Z, Zhu X, Yang Y.(2017).Chemical Synthesis of the ODM-201's Diastereomers through an Efficient Intramolecular 1,3-Dipolar Cycloaddition.Chem Pharm Bull (Tokyo).Jun 1;65(6):582-585
- General References
- Shore N, Zurth C, Fricke R, Gieschen H, Graudenz K, Koskinen M, Ploeger B, Moss J, Prien O, Borghesi G, Petrenciuc O, Tammela TL, Kuss I, Verholen F, Smith MR, Fizazi K: Evaluation of Clinically Relevant Drug-Drug Interactions and Population Pharmacokinetics of Darolutamide in Patients with Nonmetastatic Castration-Resistant Prostate Cancer: Results of Pre-Specified and Post Hoc Analyses of the Phase III ARAMIS Trial. Target Oncol. 2019 Oct;14(5):527-539. doi: 10.1007/s11523-019-00674-0. [Article]
- Matsubara N, Mukai H, Hosono A, Onomura M, Sasaki M, Yajima Y, Hashizume K, Yasuda M, Uemura M, Zurth C: Phase 1 study of darolutamide (ODM-201): a new-generation androgen receptor antagonist, in Japanese patients with metastatic castration-resistant prostate cancer. Cancer Chemother Pharmacol. 2017 Dec;80(6):1063-1072. doi: 10.1007/s00280-017-3417-3. Epub 2017 Aug 11. [Article]
- Bastos DA, Antonarakis ES: Darolutamide For Castration-Resistant Prostate Cancer. Onco Targets Ther. 2019 Oct 23;12:8769-8777. doi: 10.2147/OTT.S197244. eCollection 2019. [Article]
- Fizazi K, Albiges L, Loriot Y, Massard C: ODM-201: a new-generation androgen receptor inhibitor in castration-resistant prostate cancer. Expert Rev Anticancer Ther. 2015;15(9):1007-17. doi: 10.1586/14737140.2015.1081566. [Article]
- Fizazi K, Smith MR, Tombal B: Clinical Development of Darolutamide: A Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer. Clin Genitourin Cancer. 2018 Oct;16(5):332-340. doi: 10.1016/j.clgc.2018.07.017. Epub 2018 Jul 24. [Article]
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use [Link]
- Darolutamide MSDS [Link]
- FDA approves darolutamide [Link]
- Darolutamide patent [Link]
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use (August 2022) [Link]
- External Links
- PubChem Compound
- 67171867
- PubChem Substance
- 347829085
- ChemSpider
- 38772320
- BindingDB
- 309979
- 2180325
- ChEMBL
- CHEMBL4297185
- Wikipedia
- Darolutamide
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Recruiting Treatment Non-Metastatic Castration-Resistant Prostate Cancer 1 3 Active Not Recruiting Treatment Neoplasms of the Prostate 1 3 Active Not Recruiting Treatment Prostate Cancer 1 3 Active Not Recruiting Treatment Prostate Carcinoma 1 3 Completed Treatment Castration Resistant Prostate Cancer / Prostate Cancer Non-Metastatic 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 300 mg Tablet, film coated Oral 300 mg/1 Tablet, film coated Oral 300 mg Tablet Oral 300.000 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8975254 No 2015-03-10 2030-10-27 US US9657003 No 2017-05-23 2030-10-27 US US10383853 No 2019-08-20 2036-01-28 US US10010530 No 2018-07-03 2036-01-28 US US10711013 No 2020-07-14 2030-10-27 US US10835515 No 2020-11-17 2036-01-28 US US11046713 No 2021-06-29 2030-10-27 US US11168058 No 2021-11-09 2038-02-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source boiling point (°C) 719.5±60.0 https://www.chemicalbook.com/ChemicalProductProperty_EN_CB43052901.htm logP 1.904 http://www.chemspider.com/Chemical-Structure.38772320.html Caco2 permeability 14 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6828636/ pKa 11.75 https://s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB12941.pdf?1577134173 - Predicted Properties
Property Value Source Water Solubility 0.0727 mg/mL ALOGPS logP 3 ALOGPS logP 2.45 Chemaxon logS -3.7 ALOGPS pKa (Strongest Acidic) 9.81 Chemaxon pKa (Strongest Basic) 2.37 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 119.62 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 117.16 m3·mol-1 Chemaxon Polarizability 41.86 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0002-0009000000-4ede44796f4f5334da5f Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-000t-6009000000-7bd98afa2abce3b2bf6e Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-000t-0549000000-cace47a46cdc932931ba Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0gcc-9566000000-9a4cd7aeb12e4900363e Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-03dj-4946000000-c4d138bb3e991d7cb6a2 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-00lu-9321000000-d509311dbbb2964680ad Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 189.22853 predictedDeepCCS 1.0 (2019) [M+H]+ 191.6241 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.6186 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Zinc ion binding
- Specific Function
- Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...
- Gene Name
- AR
- Uniprot ID
- P10275
- Uniprot Name
- Androgen receptor
- Molecular Weight
- 98987.9 Da
References
- Shore N, Zurth C, Fricke R, Gieschen H, Graudenz K, Koskinen M, Ploeger B, Moss J, Prien O, Borghesi G, Petrenciuc O, Tammela TL, Kuss I, Verholen F, Smith MR, Fizazi K: Evaluation of Clinically Relevant Drug-Drug Interactions and Population Pharmacokinetics of Darolutamide in Patients with Nonmetastatic Castration-Resistant Prostate Cancer: Results of Pre-Specified and Post Hoc Analyses of the Phase III ARAMIS Trial. Target Oncol. 2019 Oct;14(5):527-539. doi: 10.1007/s11523-019-00674-0. [Article]
- Matsubara N, Mukai H, Hosono A, Onomura M, Sasaki M, Yajima Y, Hashizume K, Yasuda M, Uemura M, Zurth C: Phase 1 study of darolutamide (ODM-201): a new-generation androgen receptor antagonist, in Japanese patients with metastatic castration-resistant prostate cancer. Cancer Chemother Pharmacol. 2017 Dec;80(6):1063-1072. doi: 10.1007/s00280-017-3417-3. Epub 2017 Aug 11. [Article]
- Fizazi K, Smith MR, Tombal B: Clinical Development of Darolutamide: A Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer. Clin Genitourin Cancer. 2018 Oct;16(5):332-340. doi: 10.1016/j.clgc.2018.07.017. Epub 2018 Jul 24. [Article]
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- Curator comments
- This target relationship has only been observed through in vitro studies. Clinical relevance is unknown.
- General Function
- Zinc ion binding
- Specific Function
- The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
- Gene Name
- PGR
- Uniprot ID
- P06401
- Uniprot Name
- Progesterone receptor
- Molecular Weight
- 98979.96 Da
References
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Zurth C, Koskinen M, Fricke R, Prien O, Korjamo T, Graudenz K, Denner K, Bairlein M, von Buhler CJ, Wilkinson G, Gieschen H: Drug-Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759. doi: 10.1007/s13318-019-00577-5. [Article]
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
- Gene Name
- UGT1A9
- Uniprot ID
- O60656
- Uniprot Name
- UDP-glucuronosyltransferase 1-9
- Molecular Weight
- 59940.495 Da
References
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- Shore N, Zurth C, Fricke R, Gieschen H, Graudenz K, Koskinen M, Ploeger B, Moss J, Prien O, Borghesi G, Petrenciuc O, Tammela TL, Kuss I, Verholen F, Smith MR, Fizazi K: Evaluation of Clinically Relevant Drug-Drug Interactions and Population Pharmacokinetics of Darolutamide in Patients with Nonmetastatic Castration-Resistant Prostate Cancer: Results of Pre-Specified and Post Hoc Analyses of the Phase III ARAMIS Trial. Target Oncol. 2019 Oct;14(5):527-539. doi: 10.1007/s11523-019-00674-0. [Article]
- Zurth C, Koskinen M, Fricke R, Prien O, Korjamo T, Graudenz K, Denner K, Bairlein M, von Buhler CJ, Wilkinson G, Gieschen H: Drug-Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759. doi: 10.1007/s13318-019-00577-5. [Article]
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Shore N, Zurth C, Fricke R, Gieschen H, Graudenz K, Koskinen M, Ploeger B, Moss J, Prien O, Borghesi G, Petrenciuc O, Tammela TL, Kuss I, Verholen F, Smith MR, Fizazi K: Evaluation of Clinically Relevant Drug-Drug Interactions and Population Pharmacokinetics of Darolutamide in Patients with Nonmetastatic Castration-Resistant Prostate Cancer: Results of Pre-Specified and Post Hoc Analyses of the Phase III ARAMIS Trial. Target Oncol. 2019 Oct;14(5):527-539. doi: 10.1007/s11523-019-00674-0. [Article]
- Zurth C, Koskinen M, Fricke R, Prien O, Korjamo T, Graudenz K, Denner K, Bairlein M, von Buhler CJ, Wilkinson G, Gieschen H: Drug-Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759. doi: 10.1007/s13318-019-00577-5. [Article]
- FDA Approved Drug Products: NUBEQA (darolutamide) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- Zurth C, Koskinen M, Fricke R, Prien O, Korjamo T, Graudenz K, Denner K, Bairlein M, von Buhler CJ, Wilkinson G, Gieschen H: Drug-Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759. doi: 10.1007/s13318-019-00577-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- Zurth C, Koskinen M, Fricke R, Prien O, Korjamo T, Graudenz K, Denner K, Bairlein M, von Buhler CJ, Wilkinson G, Gieschen H: Drug-Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759. doi: 10.1007/s13318-019-00577-5. [Article]
Drug created at October 21, 2016 01:30 / Updated at December 05, 2023 12:31