Stem definition | Drug id | CAS RN |
---|---|---|
non-steroid antiandrogens | 1223 | 13311-84-7 |
Dose | Unit | Route |
---|---|---|
0.75 | g | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 0.01 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 38.79 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
Jan. 27, 1989 | FDA |
None
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Osteonecrosis of jaw | 116.73 | 23.87 | 40 | 1433 | 16470 | 29556584 |
Prostatic specific antigen increased | 102.84 | 23.87 | 34 | 1439 | 12530 | 29560524 |
Metastases to bone | 66.05 | 23.87 | 23 | 1450 | 9875 | 29563179 |
Hormone-refractory prostate cancer | 47.72 | 23.87 | 10 | 1463 | 619 | 29572435 |
Prostate cancer | 36.50 | 23.87 | 20 | 1453 | 25507 | 29547547 |
Interstitial lung disease | 27.84 | 23.87 | 23 | 1450 | 57695 | 29515359 |
Traumatic fracture | 24.73 | 23.87 | 5 | 1468 | 259 | 29572795 |
Taste disorder | 23.96 | 23.87 | 9 | 1464 | 4767 | 29568287 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Prostatic specific antigen increased | 131.83 | 28.07 | 32 | 1401 | 8728 | 64488571 |
Osteonecrosis of jaw | 106.25 | 28.07 | 38 | 1395 | 39787 | 64457512 |
Hormone-refractory prostate cancer | 61.03 | 28.07 | 10 | 1423 | 362 | 64496937 |
Metastases to bone | 52.52 | 28.07 | 19 | 1414 | 20416 | 64476883 |
Prostate cancer | 42.03 | 28.07 | 16 | 1417 | 19779 | 64477520 |
Taste disorder | 28.90 | 28.07 | 10 | 1423 | 9423 | 64487876 |
None
Source | Code | Description |
---|---|---|
ATC | L02BB01 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Anti-androgens |
FDA MoA | N0000000243 | Androgen Receptor Antagonists |
FDA EPC | N0000175560 | Androgen Receptor Inhibitor |
CHEBI has role | CHEBI:35497 | antiandrogen |
CHEBI has role | CHEBI:35610 | antineoplastic agents |
MeSH PA | D000726 | Androgen Antagonists |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D018931 | Antineoplastic Agents, Hormonal |
MeSH PA | D006727 | Hormone Antagonists |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Neoplasm of prostate | indication | 126906006 | DOID:10283 |
Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
Methemoglobinemia | contraindication | 38959009 | DOID:10783 |
Hepatic failure | contraindication | 59927004 | |
Anemia due to enzyme deficiency | contraindication | 111577008 | |
Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
Deficiency of cytochrome-b>5< reductase | contraindication | 124184009 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Pregnancy, function | contraindication | 289908002 | |
Breastfeeding (mother) | contraindication | 413712001 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.76 | acidic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Androgen receptor | Nuclear hormone receptor | ANTAGONIST | Ki | 5.89 | CHEMBL | CHEMBL | |||
5-hydroxytryptamine receptor 6 | GPCR | Ki | 5.08 | DRUG MATRIX | |||||
Cytochrome P450 1A2 | Enzyme | Ki | 5.36 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 4 | GPCR | Ki | 5.65 | DRUG MATRIX | |||||
Androgen receptor | Transcription factor | Ki | 5.05 | DRUG MATRIX | |||||
Bile salt export pump | Transporter | IC50 | 4.10 | CHEMBL |
ID | Source |
---|---|
4019377 | VUID |
N0000147534 | NUI |
D00586 | KEGG_DRUG |
4019377 | VANDF |
C0016384 | UMLSCUI |
CHEBI:5132 | CHEBI |
CHEMBL806 | ChEMBL_ID |
DB00499 | DRUGBANK_ID |
D005485 | MESH_DESCRIPTOR_UI |
3397 | PUBCHEM_CID |
6943 | IUPHAR_LIGAND_ID |
3483 | INN_ID |
76W6J0943E | UNII |
4508 | RXNORM |
42238 | MMSL |
4755 | MMSL |
d00240 | MMSL |
002677 | NDDF |
387587007 | SNOMEDCT_US |
96371003 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Flutamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49884-753 | CAPSULE | 125 mg | ORAL | ANDA | 17 sections |
Flutamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60429-272 | CAPSULE | 125 mg | ORAL | ANDA | 17 sections |
FLUTAMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-915 | CAPSULE | 125 mg | ORAL | ANDA | 20 sections |
Eulexin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 80725-600 | CAPSULE | 125 mg | ORAL | ANDA | 26 sections |