lomustine ๐Ÿถ Veterinary Use | 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 ยตM/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
Tumour pseudoprogression 63.65 33.15 10 1389 220 50603505
Platelet count decreased 61.92 33.15 37 1362 100689 50503036
Ototoxicity 53.61 33.15 11 1388 1116 50602609
Full blood count abnormal 46.00 33.15 19 1380 23369 50580356
Geotrichum infection 43.42 33.15 8 1391 462 50603263
Mucosal inflammation 42 33.15 21 1378 40121 50563604
Nausea 37.30 33.15 68 1331 705330 49898395
Thrombocytopenia 35.84 33.15 29 1370 127644 50476081
Disease progression 33.94 33.15 25 1374 95841 50507884
Death 33.69 33.15 43 1356 325336 50278389

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
Disease progression 59.51 30.10 47 1951 81869 29490660
Aeromonas infection 53.60 30.10 10 1988 247 29572282
Second primary malignancy 45.15 30.10 17 1981 6688 29565841
Nausea 39.51 30.10 70 1928 289185 29283344
Tumour pseudoprogression 32.37 30.10 7 1991 369 29572160
Platelet count decreased 31.53 30.10 37 1961 104635 29467894
Fatigue 31.39 30.10 67 1931 316754 29255775

FDA Adverse Event Reporting System (Geriatric)

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
Tumour pseudoprogression 95.55 29.04 17 2877 490 64495348
Disease progression 81.55 29.04 60 2834 141620 64354218
Platelet count decreased 58.34 29.04 53 2841 167658 64328180
Aeromonas infection 54.86 29.04 10 2884 331 64495507
Acute myeloid leukaemia 51.58 29.04 25 2869 27438 64468400
Geotrichum infection 50.52 29.04 11 2883 907 64494931
Seizure 48.95 29.04 48 2846 166844 64328994
Second primary malignancy 45.28 29.04 18 2876 12319 64483519
Ototoxicity 43.19 29.04 12 2882 2711 64493127
Off label use 36.05 29.04 84 2810 632722 63863116
Death 35.38 29.04 71 2823 482634 64013204
Thrombocytopenia 34.27 29.04 46 2848 223755 64272083
Malignant neoplasm progression 34.05 29.04 33 2861 112838 64383000

FDA Adverse Event Reporting System (Pediatric)

None

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
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018906 Antineoplastic Agents, Alkylating
MeSH PA D009676 Noxae
CHEBI has role CHEBI:35610 antineoplastic agents

Drug Use | Suggest Off label Use Form| |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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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:

None

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Gleostine HUMAN PRESCRIPTION DRUG LABEL 1 58181-3040 CAPSULE, GELATIN COATED 10 mg ORAL NDA 24 sections
Gleostine HUMAN PRESCRIPTION DRUG LABEL 1 58181-3041 CAPSULE, GELATIN COATED 40 mg ORAL NDA 24 sections
Gleostine HUMAN PRESCRIPTION DRUG LABEL 1 58181-3042 CAPSULE, GELATIN COATED 100 mg ORAL NDA 24 sections