clevidipine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 674 167221-71-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • clevidipine
  • clevelox
  • cleviprex
a calcium channel blocker and antihypertensive agent
  • Molecular weight: 456.32
  • Formula: C21H23Cl2NO6
  • CLOGP: 5.53
  • LIPINSKI: 1
  • HAC: 7
  • HDO: 1
  • TPSA: 90.93
  • ALOGS: -5.23
  • ROTB: 10

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.65 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.58 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 142 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.30 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 1, 2008 FDA MEDICINES CO

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C08CA16 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
FDA CS M0006414 Dihydropyridines
FDA MoA N0000000069 Calcium Channel Antagonists
FDA EPC N0000175421 Dihydropyridine Calcium Channel Blocker
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Tachyarrhythmia contraindication 6285003
Minimal change disease contraindication 44785005 DOID:10966
Low blood pressure contraindication 45007003
Pancreatitis contraindication 75694006 DOID:4989
Heart failure contraindication 84114007 DOID:6000
Hypertriglyceridemia contraindication 302870006
Severe Aortic Valve Stenosis contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 0.56 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel BLOCKER WOMBAT-PK CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel BLOCKER WOMBAT-PK CHEMBL

External reference:

IDSource
4028719 VUID
N0000178415 NUI
D08892 KEGG_DRUG
4028719 VANDF
C2981161 UMLSCUI
CHEBI:135738 CHEBI
CHEMBL1237132 ChEMBL_ID
DB04920 DRUGBANK_ID
C118563 MESH_SUPPLEMENTAL_RECORD_UI
153994 PUBCHEM_CID
7468 IUPHAR_LIGAND_ID
7490 INN_ID
19O2GP3B7Q UNII
233603 RXNORM
147455 MMSL
d07312 MMSL
012824 NDDF
439471002 SNOMEDCT_US
439624003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cleviprex HUMAN PRESCRIPTION DRUG LABEL 1 10122-610 EMULSION 0.50 mg INTRAVENOUS NDA 25 sections
Cleviprex HUMAN PRESCRIPTION DRUG LABEL 1 10122-611 EMULSION 0.50 mg INTRAVENOUS NDA 25 sections
Cleviprex HUMAN PRESCRIPTION DRUG LABEL 1 18124-011 EMULSION 0.50 mg INTRAVENOUS NDA 28 sections