General Information of Drug (ID: DMZMSPF)

Drug Name
Bicalutamide
Synonyms
Casodex; Cosudex; Propanamide; Raffolutil; Astra brand of bicalutamide; AstraZeneca brand of bicalutamide; Zeneca brand of bicalutamide; Calutide (TN); Casodex (TN); Cosudex (TN); KS-1161; Kalumid (TN); Bicalutamide [USAN:INN:BAN]; Bicalutamide (JAN/USP/INN); Casodex, Cosudex, Calutide, Kalumid, Bicalutamide; N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide; (+-)-4'-Cyano-alpha,alpha,alpha-trifluoro-3-((p-fluorophenyl)sulfonyl)-2-methyl-m-lactotoluidide; 4'-cyano-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methyl-3'-(trifluoromethyl)propionanilide
Indication
Disease Entry ICD 11 Status REF
Prostate cancer 2C82.0 Approved [1], [2]
Therapeutic Class
Anticancer Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 430.4
Topological Polar Surface Area (xlogp) 2.3
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 9
ADMET Property
Absorption
The drug is well-absorbed following oral administration [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Clearance
The apparent oral clearance of drug is 0.32 L/h [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 5.9 days [6]
Metabolism
The drug is metabolized via the glucuronidation [3]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.93549 micromolar/kg/day [7]
Water Solubility
The ability of drug to dissolve in water is measured as 0.005 mg/mL [4]
Chemical Identifiers
Formula
C18H14F4N2O4S
IUPAC Name
N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide
Canonical SMILES
CC(CS(=O)(=O)C1=CC=C(C=C1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O
InChI
InChI=1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)
InChIKey
LKJPYSCBVHEWIU-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
2375
ChEBI ID
CHEBI:91617
CAS Number
90357-06-5
DrugBank ID
DB01128
TTD ID
D0V9BD
VARIDT ID
DR00795
INTEDE ID
DR0210
ACDINA ID
D00069

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Androgen receptor (AR) TTS64P2 ANDR_HUMAN Antagonist [8], [9]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [10]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [10]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [11]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Prostate cancer
ICD Disease Classification 2C82.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Androgen receptor (AR) DTT AR 2.13E-01 -0.07 -0.11
P-glycoprotein 1 (ABCB1) DTP P-GP 2.80E-02 -1.36E-01 -1.05E+00
Breast cancer resistance protein (ABCG2) DTP BCRP 1.91E-02 2.50E-01 1.01E+00
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 7.93E-02 -8.20E-02 -8.93E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Bicalutamide (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Bicalutamide and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [46]
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Bicalutamide and Ivosidenib. Acute myeloid leukaemia [2A60] [47]
Midostaurin DMI6E0R Moderate Decreased metabolism of Bicalutamide caused by Midostaurin mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [48]
Idarubicin DMM0XGL Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Idarubicin. Acute myeloid leukaemia [2A60] [49]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Gilteritinib. Acute myeloid leukaemia [2A60] [49]
Oliceridine DM6MDCF Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Oliceridine. Acute pain [MG31] [49]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Ivabradine. Angina pectoris [BA40] [49]
Bepridil DM0RKS4 Major Increased risk of prolong QT interval by the combination of Bicalutamide and Bepridil. Angina pectoris [BA40] [50]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Bicalutamide and Dronedarone. Angina pectoris [BA40] [50]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Bicalutamide and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [51]
Cilostazol DMZMSCT Moderate Decreased metabolism of Bicalutamide caused by Cilostazol mediated inhibition of CYP450 enzyme. Arterial occlusive disease [BD40] [52]
Posaconazole DMUL5EW Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Posaconazole. Aspergillosis [1F20] [49]
Levalbuterol DM5YBO1 Moderate Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Levalbuterol. Asthma [CA23] [53]
Pirbuterol DMI5678 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Pirbuterol. Asthma [CA23] [54]
Budesonide DMJIBAW Moderate Decreased metabolism of Bicalutamide caused by Budesonide mediated inhibition of CYP450 enzyme. Asthma [CA23] [55]
Lisdexamfetamine DM6W8V5 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [49]
Desipramine DMT2FDC Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Desipramine. Attention deficit hyperactivity disorder [6A05] [49]
Ofloxacin DM0VQN3 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Ofloxacin. Bacterial infection [1A00-1C4Z] [49]
Clarithromycin DM4M1SG Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Clarithromycin. Bacterial infection [1A00-1C4Z] [49]
Sparfloxacin DMB4HCT Major Increased risk of prolong QT interval by the combination of Bicalutamide and Sparfloxacin. Bacterial infection [1A00-1C4Z] [56]
Levofloxacin DMS60RB Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Levofloxacin. Bacterial infection [1A00-1C4Z] [49]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Retigabine. Behcet disease [4A62] [49]
Cariprazine DMJYDVK Moderate Decreased metabolism of Bicalutamide caused by Cariprazine mediated inhibition of CYP450 enzyme. Bipolar disorder [6A60] [49]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Bicalutamide and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [57]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Eribulin. Breast cancer [2C60-2C6Y] [49]
Ixabepilone DM2OZ3G Moderate Decreased metabolism of Bicalutamide caused by Ixabepilone mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [58]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Bosutinib. Breast cancer [2C60-2C6Y] [49]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [49]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Olodaterol. Chronic obstructive pulmonary disease [CA22] [54]
Vilanterol DMF5EK1 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Vilanterol. Chronic obstructive pulmonary disease [CA22] [53]
Indacaterol DMQJHR7 Moderate Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Indacaterol. Chronic obstructive pulmonary disease [CA22] [54]
Arformoterol DMYM974 Moderate Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Arformoterol. Chronic obstructive pulmonary disease [CA22] [54]
Halothane DM80OZ5 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Halothane. Corneal disease [9A76-9A78] [49]
Probucol DMVZQ2M Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Probucol. Coronary atherosclerosis [BA80] [49]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Bicalutamide and Pasireotide. Cushing syndrome [5A70] [50]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Osilodrostat. Cushing syndrome [5A70] [49]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Bicalutamide caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [59]
Clomipramine DMINRKW Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Clomipramine. Depression [6A70-6A7Z] [49]
Doxepin DMPI98T Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Doxepin. Depression [6A70-6A7Z] [49]
Polatuzumab vedotin DMF6Y0L Moderate Decreased metabolism of Bicalutamide caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [60]
Tetrabenazine DMYWQ0O Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [49]
Deutetrabenazine DMUPFLI Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Deutetrabenazine. Dystonic disorder [8A02] [49]
Ingrezza DMVPLNC Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Ingrezza. Dystonic disorder [8A02] [49]
Stiripentol DMMSDOY Moderate Decreased metabolism of Bicalutamide caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [49]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Bicalutamide and Cannabidiol. Epileptic encephalopathy [8A62] [49]
Solifenacin DMG592Q Moderate Decreased metabolism of Bicalutamide caused by Solifenacin mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [61]
Mirabegron DMS1GYT Minor Decreased metabolism of Bicalutamide caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [62]
Ripretinib DM958QB Moderate Decreased metabolism of Bicalutamide caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [46]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Sunitinib. Gastrointestinal stromal tumour [2B5B] [49]
Avapritinib DMK2GZX Moderate Decreased metabolism of Bicalutamide caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [49]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Bicalutamide and Brentuximab vedotin. Hodgkin lymphoma [2B30] [63]
MK-1439 DM215WE Minor Decreased metabolism of Bicalutamide caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [64]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [49]
Saquinavir DMG814N Major Increased risk of prolong QT interval by the combination of Bicalutamide and Saquinavir. Human immunodeficiency virus disease [1C60-1C62] [65]
Lopinavir DMITQS0 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Lopinavir. Human immunodeficiency virus disease [1C60-1C62] [49]
Maraviroc DMTL94F Moderate Decreased metabolism of Bicalutamide caused by Maraviroc mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [66]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Bicalutamide and Mipomersen. Hyper-lipoproteinaemia [5C80] [67]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Bicalutamide and Teriflunomide. Hyper-lipoproteinaemia [5C80] [50]
BMS-201038 DMQTAGO Major Decreased metabolism of Bicalutamide caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [68]
Retapamulin DM9JXB7 Minor Decreased metabolism of Bicalutamide caused by Retapamulin mediated inhibition of CYP450 enzyme. Impetigo [1B72] [69]
Suvorexant DM0E6S3 Moderate Decreased metabolism of Bicalutamide caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [46]
Tasimelteon DMLOQ1V Moderate Decreased metabolism of Bicalutamide caused by Tasimelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [70]
ITI-007 DMUQ1DO Moderate Decreased metabolism of Bicalutamide caused by ITI-007 mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [71]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Polyethylene glycol. Irritable bowel syndrome [DD91] [49]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Phenolphthalein. Irritable bowel syndrome [DD91] [50]
Naloxegol DML0B41 Minor Decreased metabolism of Bicalutamide caused by Naloxegol mediated inhibition of CYP450 enzyme. Large intestine motility disorder [DB32] [72]
Pemigatinib DM819JF Moderate Decreased metabolism of Bicalutamide caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [49]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Bicalutamide and Crizotinib. Lung cancer [2C25] [73]
Brigatinib DM7W94S Moderate Decreased metabolism of Bicalutamide caused by Brigatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [46]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Bicalutamide and Ceritinib. Lung cancer [2C25] [50]
Lurbinectedin DMEFRTZ Moderate Decreased metabolism of Bicalutamide caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [74]
PF-06463922 DMKM7EW Moderate Decreased metabolism of Bicalutamide caused by PF-06463922 mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [75]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Bicalutamide and Osimertinib. Lung cancer [2C25] [76]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Bicalutamide caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [77]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Bicalutamide and Selpercatinib. Lung cancer [2C25] [49]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Bicalutamide and Lumefantrine. Malaria [1F40-1F45] [46]
Halofantrine DMOMK1V Major Increased risk of prolong QT interval by the combination of Bicalutamide and Halofantrine. Malaria [1F40-1F45] [78]
Hydroxychloroquine DMSIVND Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Hydroxychloroquine. Malaria [1F40-1F45] [49]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [49]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Bicalutamide and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [79]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Bicalutamide and Idelalisib. Mature B-cell leukaemia [2A82] [80]
GDC-0199 DMH0QKA Moderate Decreased metabolism of Bicalutamide caused by GDC-0199 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [46]
Arsenic trioxide DM61TA4 Major Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Arsenic trioxide. Mature B-cell lymphoma [2A85] [81]
Acalabrutinib DM7GCVW Moderate Decreased metabolism of Bicalutamide caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [82]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Bicalutamide and Vemurafenib. Melanoma [2C30] [50]
Selumetinib DMC7W6R Moderate Decreased metabolism of Bicalutamide caused by Selumetinib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [83]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and LGX818. Melanoma [2C30] [49]
Ubrogepant DM749I3 Moderate Decreased metabolism of Bicalutamide caused by Ubrogepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [84]
Flibanserin DM70DTN Moderate Decreased metabolism of Bicalutamide caused by Flibanserin mediated inhibition of CYP450 enzyme. Mood disorder [6A60-6E23] [85]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Siponimod. Multiple sclerosis [8A40] [46]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Fingolimod. Multiple sclerosis [8A40] [50]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Bicalutamide and Ozanimod. Multiple sclerosis [8A40] [86]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Romidepsin. Mycosis fungoides [2B01] [49]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Bicalutamide and Nilotinib. Myeloproliferative neoplasm [2A20] [50]
Ruxolitinib DM7Q98D Minor Decreased metabolism of Bicalutamide caused by Ruxolitinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [49]
Dasatinib DMJV2EK Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Dasatinib. Myeloproliferative neoplasm [2A20] [49]
Entrectinib DMMPTLH Moderate Decreased metabolism of Bicalutamide caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [87]
Levomethadyl Acetate DM06HG5 Major Decreased metabolism of Bicalutamide caused by Levomethadyl Acetate mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [88]
Lofexidine DM1WXA6 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Lofexidine. Opioid use disorder [6C43] [49]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Rucaparib. Ovarian cancer [2C73] [49]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Triclabendazole. Parasitic worm infestation [1F90] [49]
Pimavanserin DMR7IVC Moderate Decreased metabolism of Bicalutamide caused by Pimavanserin mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [89]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Bicalutamide and Macimorelin. Pituitary gland disorder [5A60-5A61] [90]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Bicalutamide and Lefamulin. Pneumonia [CA40] [91]
Ergonovine DM0VEC1 Moderate Decreased metabolism of Bicalutamide caused by Ergonovine mediated inhibition of CYP450 enzyme. Postpartum haemorrhage [JA43] [92]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Bicalutamide caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [93]
Silodosin DMJSBT6 Moderate Decreased metabolism of Bicalutamide caused by Silodosin mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [94]
Everolimus DM8X2EH Moderate Decreased metabolism of Bicalutamide caused by Everolimus mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [95]
Axitinib DMGVH6N Moderate Decreased metabolism of Bicalutamide caused by Axitinib mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [49]
Temsirolimus DMS104F Moderate Decreased metabolism of Bicalutamide caused by Temsirolimus mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [96]
Aripiprazole DM3NUMH Moderate Decreased metabolism of Bicalutamide caused by Aripiprazole mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [46]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Bicalutamide and Iloperidone. Schizophrenia [6A20] [50]
Paliperidone DM7NPJS Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Paliperidone. Schizophrenia [6A20] [49]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Bicalutamide and Amisulpride. Schizophrenia [6A20] [97]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Asenapine. Schizophrenia [6A20] [49]
LDE225 DMM9F25 Moderate Decreased metabolism of Bicalutamide caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [98]
Larotrectinib DM26CQR Moderate Decreased metabolism of Bicalutamide caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [46]
Docetaxel DMDI269 Moderate Decreased metabolism of Bicalutamide caused by Docetaxel mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [99]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Bicalutamide and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [49]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Bicalutamide and LEE011. Solid tumour/cancer [2A00-2F9Z] [50]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Bicalutamide and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [50]
Taxol DMUOT9V Moderate Decreased metabolism of Bicalutamide caused by Taxol mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [100]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Pitolisant. Somnolence [MG42] [49]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [49]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Bicalutamide caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [101]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Lenvatinib. Thyroid cancer [2D10] [49]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Bicalutamide and Cabozantinib. Thyroid cancer [2D10] [49]
Saxagliptin DMGXENV Moderate Decreased metabolism of Bicalutamide caused by Saxagliptin mediated inhibition of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [49]
Elagolix DMB2C0E Moderate Decreased metabolism of Bicalutamide caused by Elagolix mediated inhibition of CYP450 enzyme. Uterine fibroid [2E86] [102]
Trimeprazine DMEMV9D Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [49]
Propafenone DMPIBJK Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Propafenone. Ventricular tachyarrhythmia [BC71] [49]
Flecainide DMSQDLE Moderate Increased risk of prolong QT interval by the combination of Bicalutamide and Flecainide. Ventricular tachyarrhythmia [BC71] [49]
⏷ Show the Full List of 132 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 300 E00651 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 4000 E00654 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Polyvinyl alcohol E00666 Not Available Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
⏷ Show the Full List of 18 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Bicalutamide 50 mg tablet 50 mg Oral Tablet Oral
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References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2863).
2 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
3 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
4 BDDCS applied to over 900 drugs
5 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
6 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
7 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
8 Androgen receptor overexpression induces tamoxifen resistance in human breast cancer cells. Breast Cancer Res Treat. 2010 May;121(1):1-11.
9 Androgen receptor as a target in androgen-independent prostate cancer. Urology. 2002 Sep;60(3 Suppl 1):132-8; discussion 138-9.
10 Effects of the ABCG2 and ABCB1 drug transporter polymorphisms on the pharmacokinetics of bicalutamide in humans. Clin Chim Acta. 2015 Jan 1;438:7-11.
11 Bicalutamide: clinical pharmacokinetics and metabolism. Clin Pharmacokinet. 2004;43(13):855-78.
12 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
13 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
14 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
15 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
16 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
17 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
18 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
19 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
20 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
21 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
22 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
23 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
24 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
25 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
26 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
27 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
28 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
29 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
30 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
31 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
32 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
33 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
34 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
35 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
36 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
37 Dehydroepiandrosterone, glucose-6-phosphate dehydrogenase, and longevity. Ageing Res Rev. 2004 Apr;3(2):171-87.
38 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
39 Molecular mechanism of androgen action. Trends Endocrinol Metab. 1998 Oct 1;9(8):317-24.
40 Ouellet M, Percival MD: Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms. Biochem J. 1995 Feb 15;306 ( Pt 1):247-51.
41 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
42 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
43 CX3CR1 is expressed by prostate epithelial cells and androgens regulate the levels of CX3CL1/fractalkine in the bone marrow: potential role in prostate cancer bone tropism. Cancer Res. 2008 Mar 15;68(6):1715-22.
44 Expression of androgen receptor on fibroblast and hepatocyte of rats after deep second-degree burn caused by scalding. Sichuan Da Xue Xue Bao Yi Xue Ban. 2005 May;36(3):362-4.
45 An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate. Endocrinology. 2007 Jan;148(1):363-73.
46 Cerner Multum, Inc. "Australian Product Information.".
47 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
48 Dutreix C, Munarini F, Lorenzo S, Roesel J, Wang Y "Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers." Cancer Chemother Pharmacol 72 (2013): 1223-34. [PMID: 24085261]
49 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
50 Canadian Pharmacists Association.
51 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
52 Hedaya MA, El-Afify DR, El-Maghraby GM "The effect of ciprofloxacin and clarithromycin on sildenafil oral bioavailability in human volunteers." Biopharm Drug Dispos 27 (2006): 103-10. [PMID: 16372380]
53 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
54 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
55 Bolland MJ, Bagg W, Thomas MG, Lucas JA, Ticehurst R, Black PN "Cushing's syndrome due to interaction between inhaled corticosteroids and itraconazole." Ann Pharmacother 38 (2004): 46-9. [PMID: 14742792]
56 Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074]
57 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
58 Product Information. Ixempra (ixabepilone). Bristol-Myers Squibb, Princeton, NJ.
59 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
60 Product Information. Polivy (polatuzumab vedotin). Genentech, South San Francisco, CA.
61 Product Information. VESIcare (solifenacin). GlaxoSmithKline, Research Triangle Park, NC.
62 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
63 Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
64 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
65 Anson BD, Weaver JG, Ackerman MJ, et al. "Blockade of HERG channels by HIV protease inhibitors." Lancet 365 (2005): 682-686. [PMID: 15721475]
66 Product Information. Selzentry (maraviroc). Pfizer U.S. Pharmaceuticals Group, New York, NY.
67 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
68 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
69 Product Information. Altabax (retapamulin topical). GlaxoSmithKline, Research Triangle Park, NC.
70 Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
71 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
72 Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
73 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
74 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
75 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
76 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
77 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
78 Abernethy DR, Wesche DL, Barbey JT, et al. "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol 51 (2001): 231-7. [PMID: 11298069]
79 Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
80 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
81 Ohnishi K, Yoshida H, Shigeno K, et al. "Prolongation of the QT interval and ventricular tachycardia in patients treated with arsenic trioxide for acute promyelocytic leukemia." Ann Intern Med 133 (2000): 881-5. [PMID: 11103058]
82 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
83 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
84 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
85 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
86 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
87 Product Information. Rozlytrek (entrectinib). Genentech, South San Francisco, CA.
88 Product Information. Orlaam (levomethadyl acetate) Roxanne Laboratories Inc, Columbus, OH.
89 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
90 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
91 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
92 Francis H, Tyndall A, Webb J "Severe vascular spasm due to erythromycin-ergotamine interaction." Clin Rheumatol 3 (1984): 243-6. [PMID: 6236021]
93 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
94 Product Information. Rapaflo (silodosin). Watson Pharmaceuticals, Corona, CA.
95 Product Information. Afinitor (everolimus). Novartis Pharmaceuticals, East Hanover, NJ.
96 Product Information. Torisel (temsirolimus). Wyeth-Ayerst Laboratories, Philadelphia, PA.
97 Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.
98 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
99 Aronson JK, Grahame-Smith DG "Clinical pharmacology: adverse drug interactions." Br Med J 282 (1981): 288-91. [PMID: 6779990]
100 Bergmann TK, Filppula AM, Launiainen T, Nielsen F, Backman J, Brosen K "Neurotoxicity and low paclitaxel clearance associated with concomitant clopidogrel therapy in a 60 year old Caucasian woman with ovarian carcinoma." Br J Clin Pharmacol (2015):. [PMID: 26446447]
101 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
102 Product Information. Orilissa (elagolix). AbbVie US LLC, North Chicago, IL.