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

Stem definition	Drug id	CAS RN
antineoplastic, alkylating agents, (beta-chloroethyl)amine derivatives	1596	13010-47-4

Description:

Molecule

Description

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:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
Aug. 4, 1976	FDA	CORDEN PHARMA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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