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

Stem definitionDrug idCAS RN
antineoplastic, alkylating agents, (beta-chloroethyl)amine derivatives 1596 13010-47-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lomustine
  • belustine
  • chloroethylcyclohexylnitrosourea
  • lomustin
An alkylating agent of value against both hematologic malignancies and solid tumors.
  • Molecular weight: 233.70
  • Formula: C9H16ClN3O2
  • CLOGP: 2.75
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 61.77
  • ALOGS: -2.49
  • ROTB: 4

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.02 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Aug. 4, 1976 FDA CORDEN PHARMA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Geotrichum infection 56.38 48.50 6 221 8 2357850
Febrile neutropenia 55.29 48.50 15 212 10867 2346991

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
ATC L01AD02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
ALKYLATING AGENTS
Nitrosoureas
FDA MoA N0000000236 Alkylating Activity
FDA EPC N0000175558 Alkylating Drug
MeSH PA D000477 Alkylating Agents
CHEBI has role CHEBI:35610 antineoplastic agent
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018906 Antineoplastic Agents, Alkylating
MeSH PA D009676 Noxae

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hodgkin's disease indication 118599009
Neoplasm of brain indication 126952004 DOID:1319
Allogeneic bone marrow transplantation off-label use 58390007
Mycosis contraindication 3218000 DOID:1564
Hyperbilirubinemia contraindication 14783006 DOID:2741
Viral disease contraindication 34014006 DOID:934
Fibrosis of lung contraindication 51615001 DOID:3770
Leukopenia contraindication 84828003 DOID:615
Bacterial infectious disease contraindication 87628006
Kidney disease contraindication 90708001 DOID:557
Bleeding contraindication 131148009
Liver function tests abnormal contraindication 166603001
Drug-induced hepatitis contraindication 235876009
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Bone marrow depression contraindication 307762000
Breastfeeding (mother) contraindication 413712001
Pulmonary Infiltrates contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.87 acidic

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
DNA DNA OTHER DRUG LABEL DRUG LABEL

External reference:

IDSource
4018138 VUID
N0000146475 NUI
C0023972 UMLSCUI
D00363 KEGG_DRUG
7BRF0Z81KG UNII
3184 INN_ID
40999006 SNOMEDCT_US
4018138 VANDF
6466 RXNORM
387227009 SNOMEDCT_US
4991 MMSL
d01341 MMSL
002639 NDDF
52513 MMSL
3950 PUBCHEM_CID
CHEBI:6520 CHEBI
CHEMBL514 ChEMBL_ID
DB01206 DRUGBANK_ID
D008130 MESH_DESCRIPTOR_UI
7214 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Gleostine HUMAN PRESCRIPTION DRUG LABEL 1 58181-3040 CAPSULE, GELATIN COATED 10 mg ORAL NDA 16 sections
Gleostine HUMAN PRESCRIPTION DRUG LABEL 1 58181-3041 CAPSULE, GELATIN COATED 40 mg ORAL NDA 16 sections
Gleostine HUMAN PRESCRIPTION DRUG LABEL 1 58181-3042 CAPSULE, GELATIN COATED 100 mg ORAL NDA 16 sections