lomustine 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 |
|---|---|
|
Synonyms:
|
An alkylating agent of value against both hematologic malignancies and solid tumors.
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 |
|---|---|---|---|---|---|---|
| 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 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 |
|---|
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 |
| 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)
| 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 |
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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| DNA | DNA | OTHER | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |