Stem definition | Drug id | CAS RN |
---|---|---|
gastrointestinal lipase inhibitors | 1996 | 96829-58-2 |
Dose | Unit | Route |
---|---|---|
0.36 | g | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 9.22 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 1 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
April 23, 1999 | FDA | HOFFMANN LA ROCHE |
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 |
---|---|---|---|---|---|---|
Steatorrhoea | 173.50 | 19.39 | 31 | 4930 | 369 | 46680732 |
Cerebral venous thrombosis | 92.94 | 19.39 | 25 | 4936 | 2102 | 46678999 |
Thalamic infarction | 68.43 | 19.39 | 15 | 4946 | 530 | 46680571 |
Drug interaction | 63.48 | 19.39 | 92 | 4869 | 203002 | 46478099 |
Cholelithiasis | 55.26 | 19.39 | 40 | 4921 | 38641 | 46642460 |
Rectal discharge | 54.61 | 19.39 | 12 | 4949 | 429 | 46680672 |
Rectal haemorrhage | 53.37 | 19.39 | 39 | 4922 | 38216 | 46642885 |
Abdominal pain | 49.58 | 19.39 | 88 | 4873 | 229943 | 46451158 |
Crystal nephropathy | 42.25 | 19.39 | 11 | 4950 | 814 | 46680287 |
Haematochezia | 38.73 | 19.39 | 32 | 4929 | 37461 | 46643640 |
Hyperoxaluria | 36.83 | 19.39 | 7 | 4954 | 119 | 46680982 |
Kidney fibrosis | 36.30 | 19.39 | 11 | 4950 | 1414 | 46679687 |
Slow response to stimuli | 32.70 | 19.39 | 9 | 4952 | 823 | 46680278 |
Nephropathy | 32.34 | 19.39 | 14 | 4947 | 4991 | 46676110 |
Oxalosis | 30.61 | 19.39 | 5 | 4956 | 33 | 46681068 |
Jaundice | 30.58 | 19.39 | 25 | 4936 | 28820 | 46652281 |
Acute hepatic failure | 30.04 | 19.39 | 19 | 4942 | 14702 | 46666399 |
Obesity | 28.15 | 19.39 | 18 | 4943 | 14188 | 46666913 |
Abdominal pain upper | 27.95 | 19.39 | 53 | 4908 | 145252 | 46535849 |
Urine oxalate increased | 27.82 | 19.39 | 6 | 4955 | 196 | 46680905 |
Renal tubular atrophy | 26.79 | 19.39 | 7 | 4954 | 525 | 46680576 |
Virologic failure | 24.70 | 19.39 | 9 | 4952 | 2046 | 46679055 |
Oropharyngeal blistering | 23.70 | 19.39 | 7 | 4954 | 825 | 46680276 |
Vanishing bile duct syndrome | 20.64 | 19.39 | 6 | 4955 | 668 | 46680433 |
Bradyphrenia | 20.59 | 19.39 | 11 | 4950 | 6219 | 46674882 |
Pregnancy on oral contraceptive | 20.44 | 19.39 | 7 | 4954 | 1327 | 46679774 |
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 |
---|---|---|---|---|---|---|
Nephropathy | 44.77 | 25.39 | 14 | 1174 | 5402 | 29945888 |
Blood uric acid increased | 43.31 | 25.39 | 14 | 1174 | 6009 | 29945281 |
Hyperoxaluria | 29.07 | 25.39 | 5 | 1183 | 134 | 29951156 |
Sleep apnoea syndrome | 26.31 | 25.39 | 13 | 1175 | 16844 | 29934446 |
Source | Code | Description |
---|---|---|
ATC | A08AB01 | ALIMENTARY TRACT AND METABOLISM ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS Peripherally acting antiobesity products |
FDA MoA | N0000009916 | Lipase Inhibitors |
FDA EPC | N0000175591 | Intestinal Lipase Inhibitor |
MeSH PA | D019440 | Anti-Obesity Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D057847 | Lipid Regulating Agents |
CHEBI has role | CHEBI:65001 | pancreatic triacylglycerol lipase inhibitor |
CHEBI has role | CHEBI:71476 | (fas) inhibitors |
CHEBI has role | CHEBI:74518 | anti-obestic agent |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Obesity | indication | 414916001 | DOID:9970 |
Primary hyperoxaluria | contraindication | 17901006 | DOID:2977 |
Obstruction of bile duct | contraindication | 30144000 | |
Anorexia nervosa | contraindication | 56882008 | DOID:8689 |
Hepatic failure | contraindication | 59927004 | |
Bulimia nervosa | contraindication | 78004001 | |
Vitamin deficiency | contraindication | 85670002 | |
Hepatic necrosis | contraindication | 87248009 | |
Liver function tests abnormal | contraindication | 166603001 | |
Drug-induced hepatitis | contraindication | 235876009 | |
Malabsorption States | contraindication | ||
Calcium Oxalate Renal Calculi | contraindication |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 13.77 | acidic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Pancreatic triacylglycerol lipase | Enzyme | INHIBITOR | IC50 | 8.90 | IUPHAR | DRUG LABEL | |||
Gastric triacylglycerol lipase | Enzyme | INHIBITOR | CHEMBL | DRUG LABEL | |||||
Monoacylglycerol lipase ABHD12 | Enzyme | IC50 | 7.10 | CHEMBL | |||||
Monoacylglycerol lipase ABHD6 | Enzyme | IC50 | 7.32 | CHEMBL | |||||
Sn1-specific diacylglycerol lipase alpha | Enzyme | IC50 | 8 | CHEMBL | |||||
Abhydrolase domain-containing protein 16A | Enzyme | IC50 | 7.52 | CHEMBL | |||||
Platelet-activating factor acetylhydrolase | Enzyme | IC50 | 7.30 | CHEMBL | |||||
Sn1-specific diacylglycerol lipase beta | Enzyme | IC50 | 7.22 | CHEMBL | |||||
Cannabinoid receptor 1 | GPCR | Ki | 5.60 | CHEMBL | |||||
Fatty-acid amide hydrolase 1 | Enzyme | IC50 | 8 | CHEMBL | |||||
Pancreatic triacylglycerol lipase | Enzyme | IC50 | 6.66 | CHEMBL |
ID | Source |
---|---|
4021159 | VUID |
N0000148610 | NUI |
D04028 | KEGG_DRUG |
4021159 | VANDF |
C1871879 | UMLSCUI |
CHEBI:94686 | CHEBI |
CHEMBL175247 | ChEMBL_ID |
D000077403 | MESH_DESCRIPTOR_UI |
3034010 | PUBCHEM_CID |
DB01083 | DRUGBANK_ID |
5277 | IUPHAR_LIGAND_ID |
6318 | INN_ID |
95M8R751W8 | UNII |
226918 | RXNORM |
109396 | MMSL |
29932 | MMSL |
8088 | MMSL |
d04429 | MMSL |
007654 | NDDF |
116093009 | SNOMEDCT_US |
387007000 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
ALLI | HUMAN OTC DRUG LABEL | 1 | 0135-0461 | CAPSULE | 60 mg | ORAL | NDA | 17 sections |
Xenical | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61269-460 | CAPSULE | 120 mg | ORAL | NDA | 31 sections |