lomustine 🐶 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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility) 0.05 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

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
Thrombocytopenia 69.29 32.12 46 1698 151111 63336167
Eastern Cooperative Oncology Group performance status worsened 64.22 32.12 13 1731 1241 63486037
Tumour pseudoprogression 61.32 32.12 10 1734 282 63486996
Platelet count decreased 57.21 32.12 37 1707 116085 63371193
Mucosal inflammation 56.61 32.12 27 1717 46901 63440377
Ototoxicity 51.59 32.12 11 1733 1351 63485927
Death 44.72 32.12 53 1691 374328 63112950
Geotrichum infection 43.40 32.12 8 1736 466 63486812
Full blood count abnormal 40.53 32.12 19 1725 31698 63455580
Nausea 40.02 32.12 78 1666 854393 62632885
Neutropenia 39.55 32.12 35 1709 174970 63312308
Disease progression 36.96 32.12 29 1715 122729 63364549
Aspergilloma 34.47 32.12 6 1738 252 63487026
Acute myeloid leukaemia 34.01 32.12 14 1730 17133 63470145
Type 2 diabetes mellitus 32.99 32.12 21 1723 63847 63423431
Bone marrow failure 32.71 32.12 16 1728 29274 63458004

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 61.19 26.25 53 2239 108024 34846615
Aeromonas infection 52.90 26.25 10 2282 274 34954365
Eastern Cooperative Oncology Group performance status worsened 45.35 26.25 11 2281 997 34953642
Second primary malignancy 42.95 26.25 17 2275 7869 34946770
Seizure 39.34 26.25 41 2251 104816 34849823
Nausea 36.47 26.25 73 2219 339835 34614804
Platelet count decreased 34.87 26.25 41 2251 119676 34834963
Fatigue 33.25 26.25 74 2218 370579 34584060
Thrombocytopenia 32.11 26.25 45 2247 156202 34798437
Tumour pseudoprogression 30.59 26.25 7 2285 493 34954146
Death 29.73 26.25 74 2218 397975 34556664
Hereditary motor and sensory neuropathy 28.30 26.25 4 2288 15 34954624
Necrotising fasciitis 27.40 26.25 10 2282 3712 34950927

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
Eastern Cooperative Oncology Group performance status worsened 110.41 28.08 24 3427 2041 79738896
Tumour pseudoprogression 91.20 28.08 17 3434 662 79740275
Disease progression 88.38 28.08 69 3382 184293 79556644
Thrombocytopenia 87.49 28.08 80 3371 265179 79475758
Seizure 60.29 28.08 56 3395 188778 79552159
Platelet count decreased 58.83 28.08 56 3395 194608 79546329
Aeromonas infection 54.24 28.08 10 3441 366 79740571
Acute myeloid leukaemia 52.59 28.08 26 3425 30859 79710078
Death 52.19 28.08 90 3361 566424 79174513
Neutropenia 51.97 28.08 63 3388 287647 79453290
Geotrichum infection 50.19 28.08 11 3440 970 79739967
Second primary malignancy 50.12 28.08 20 3431 14330 79726607
Ototoxicity 41.43 28.08 12 3439 3262 79737675
Off label use 38.19 28.08 105 3346 907110 78833827
Malignant neoplasm progression 37.05 28.08 37 3414 135953 79604984
Neoplasm progression 32.90 28.08 23 3428 51659 79689278
Product use in unapproved indication 31.53 28.08 46 3405 250313 79490624
Type 2 diabetes mellitus 28.62 28.08 22 3429 57100 79683837
Bone marrow failure 28.53 28.08 21 3430 51086 79689851
Myelosuppression 28.17 28.08 19 3432 40277 79700660

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




🐶 Veterinary Drug Use

None

🐶 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
7214 IUPHAR_LIGAND_ID
3184 INN_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 58181-3040 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 58181-3041 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
Gleostine HUMAN PRESCRIPTION DRUG LABEL 1 58181-3042 CAPSULE, GELATIN COATED 100 mg ORAL NDA 24 sections