cerivastatin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihyperlipidaemic substances, HMG CoA reductase inhibitors | 577 | 145599-86-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Cerivastatin is a competitive inhibitor of HMG-CoA reductase, which is responsible for the conversion of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) to mevalonate, a precursor of sterols, including cholesterol. The inhibition of cholesterol biosynthesis by cerivastatin reduces the level of cholesterol in hepatic cells, which stimulates the synthesis of LDL receptors, thereby increasing the uptake of cellular LDL particles. The end result of these biochemical processes is a reduction of the plasma cholesterol concentration.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 195 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 24 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.01 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 60 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.33 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.90 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.01 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.80 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 26, 1997 | FDA | BAYER PHARMS |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C10AA06 | CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN HMG CoA reductase inhibitors |
| MeSH PA | D000924 | Anticholesteremic Agents |
| MeSH PA | D000963 | Antimetabolites |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D019161 | Hydroxymethylglutaryl-CoA Reductase Inhibitors |
| MeSH PA | D000960 | Hypolipidemic Agents |
| MeSH PA | D057847 | Lipid Regulating Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypercholesterolemia | indication | 13644009 | |
| Mixed hyperlipidemia | indication | 267434003 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Hemorrhagic cerebral infarction | contraindication | 230706003 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Rhabdomyolysis | contraindication | 240131006 | |
| Pregnancy, function | contraindication | 289908002 | |
| Breastfeeding (mother) | contraindication | 413712001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.05 | acidic |
| pKa2 | 13.1 | acidic |
| pKa3 | 13.99 | acidic |
| pKa4 | 5.78 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Enzyme | INHIBITOR | IC50 | 8 | WOMBAT-PK | CHEMBL | |||
| Nuclear receptor subfamily 1 group I member 3 | Nuclear hormone receptor | WOMBAT-PK | |||||||
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Enzyme | IC50 | 8.55 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021111 | VUID |
| N0000148566 | NUI |
| D00889 | KEGG_DRUG |
| 143201-11-0 | SECONDARY_CAS_RN |
| 215567 | RXNORM |
| C0528023 | UMLSCUI |
| CHEBI:3558 | CHEBI |
| 116 | PDB_CHEM_ID |
| CHEMBL1477 | ChEMBL_ID |
| CHEMBL1200563 | ChEMBL_ID |
| DB00439 | DRUGBANK_ID |
| C086276 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2950 | IUPHAR_LIGAND_ID |
| 7083 | INN_ID |
| AM91H2KS67 | UNII |
| 446156 | PUBCHEM_CID |
| 11450 | MMSL |
| 4398 | MMSL |
| d04140 | MMSL |
| 006489 | NDDF |
| 006490 | NDDF |
| 108596008 | SNOMEDCT_US |
| 108597004 | SNOMEDCT_US |
| 373443008 | SNOMEDCT_US |
| 4021111 | VANDF |
| 4024119 | VANDF |
Pharmaceutical products:
None