Stem definition | Drug id | CAS RN |
---|---|---|
arotinoid derivatives | 361 | 153559-49-0 |
None
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 0.01 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 28.70 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Date | Agency | Company | Orphan |
---|---|---|---|
March 29, 2001 | EMA | ||
Dec. 29, 1999 | FDA | VALEANT LUXEMBOURG |
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 |
---|---|---|---|---|---|---|
Cutaneous T-cell lymphoma | 78.03 | 35.67 | 13 | 399 | 1350 | 46684300 |
Hypertriglyceridaemia | 76.55 | 35.67 | 16 | 396 | 5688 | 46679962 |
Diffuse large B-cell lymphoma | 37.47 | 35.67 | 9 | 403 | 5929 | 46679721 |
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 |
---|---|---|---|---|---|---|
Hypothyroidism | 118.50 | 28.91 | 34 | 759 | 14929 | 29936756 |
Hypertriglyceridaemia | 104.24 | 28.91 | 27 | 766 | 8071 | 29943614 |
Cutaneous T-cell lymphoma | 88.21 | 28.91 | 17 | 776 | 1318 | 29950367 |
Dyslipidaemia | 40.70 | 28.91 | 12 | 781 | 5715 | 29945970 |
Thyroid stimulating hormone deficiency | 31.94 | 28.91 | 4 | 789 | 15 | 29951670 |
Source | Code | Description |
---|---|---|
ATC | L01XF03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Retinoids for cancer treatment |
FDA CS | M0018962 | Retinoids |
FDA EPC | N0000175607 | Retinoid |
MeSH PA | D000970 | Antineoplastic Agents |
CHEBI has role | CHEBI:35610 | cytostatic |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Primary cutaneous T-cell lymphoma | indication | 400122007 | |
Alcoholism | contraindication | 7200002 | |
Hypothyroidism | contraindication | 40930008 | DOID:1459 |
Hepatic failure | contraindication | 59927004 | |
Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
Leukopenia | contraindication | 84828003 | DOID:615 |
Bilateral cataracts | contraindication | 95722004 | |
Disorder of biliary tract | contraindication | 105997008 | DOID:9741 |
Acute pancreatitis | contraindication | 197456007 | DOID:2913 |
Chronic pancreatitis | contraindication | 235494005 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Diabetic - poor control | contraindication | 268519009 | |
Pregnancy, function | contraindication | 289908002 | |
Breastfeeding (mother) | contraindication | 413712001 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 4.23 | acidic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Retinoic acid receptor RXR-alpha | Nuclear hormone receptor | AGONIST | Kd | 7.85 | CHEMBL | CHEMBL | |||
Retinoic acid receptor RXR-beta | Nuclear hormone receptor | AGONIST | Ki | 8.23 | CHEMBL | CHEMBL | |||
Retinoic acid receptor RXR-gamma | Nuclear hormone receptor | AGONIST | Ki | 8.08 | CHEMBL | CHEMBL | |||
Retinoic acid receptor beta | Nuclear hormone receptor | Ki | 7.30 | CHEMBL | |||||
Retinoic acid receptor alpha | Nuclear hormone receptor | Ki | 6.74 | CHEMBL | |||||
Retinoic acid receptor gamma | Nuclear hormone receptor | Ki | 6.89 | CHEMBL | |||||
Peroxisome proliferator-activated receptor gamma | Nuclear hormone receptor | ANTAGONIST | IC50 | 5.52 | IUPHAR | ||||
Retinoic acid receptor RXR-gamma | Transcription factor | Kd | 7.54 | CHEMBL | |||||
Retinoic acid receptor RXR-alpha | Transcription factor | EC50 | 7.40 | CHEMBL | |||||
Retinoic acid receptor RXR-alpha | Unclassified | EC50 | 7.40 | CHEMBL | |||||
Retinoic acid receptor RXR-beta | Transcription factor | Kd | 7.68 | CHEMBL |
ID | Source |
---|---|
A61RXM4375 | UNII |
4021197 | VUID |
N0000148643 | NUI |
D03106 | KEGG_DRUG |
4021197 | VANDF |
C0765273 | UMLSCUI |
CHEBI:50859 | CHEBI |
9RA | PDB_CHEM_ID |
CHEMBL1023 | ChEMBL_ID |
DB00307 | DRUGBANK_ID |
D000077610 | MESH_DESCRIPTOR_UI |
7782 | INN_ID |
82146 | PUBCHEM_CID |
2807 | IUPHAR_LIGAND_ID |
233272 | RXNORM |
234760 | MMSL |
31640 | MMSL |
8604 | MMSL |
d04507 | MMSL |
008004 | NDDF |
116346006 | SNOMEDCT_US |
387023000 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0399 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 25 sections |
Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5525 | GEL | 1 g | TOPICAL | NDA | 20 sections |
Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5526 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | NDA | 25 sections |
Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-6955 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 28 sections |
Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-0285 | CAPSULE | 75 mg | ORAL | ANDA | 28 sections |
Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43975-315 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 27 sections |
bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-003 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | NDA authorized generic | 25 sections |
Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1250 | CAPSULE | 75 mg | ORAL | ANDA | 27 sections |