altretamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 141 | 645-05-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The precise mechanism by which altretamine capsules exerts its cytotoxic effect is unknown, although a number of theoretical possibilities have been studied. Structurally, altretamine capsules resembles the alkylating agent triethylenemelamine, yet in vitro tests for alkylating activity of altretamine capsules and its metabolites have been negative. Altretamine capsules has been demonstrated to be efficacious for certain ovarian tumors resistant to classical alkylating agents. Metabolism of altretamine is a requirement for cytotoxicity. Synthetic monohydroxymethylmelamines, and products of altretamine metabolism, in vitro and in vivo, can form covalent adducts with tissue macromolecules including DNA, but the relevance of these reactions to antitumor activity is unknown.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 25.73 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| fu (Fraction unbound in plasma) | 0.11 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 26, 1990 | FDA | EISAI INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XX03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| 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 |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Malignant tumor of ovary | indication | 363443007 | DOID:2394 |
| Mood swings | contraindication | 18963009 | |
| Ataxia | contraindication | 20262006 | |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Peripheral nerve disease | contraindication | 302226006 | |
| Bone marrow depression | contraindication | 307762000 | |
| Vertigo | contraindication | 399153001 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Unconscious | contraindication | 418107008 | |
| Severe Bone Marrow Depression | 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 | 5.66 | Basic |
| pKa2 | 3.04 | Basic |
| pKa3 | 0.46 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Enzyme | IC50 | 5.40 | DRUG MATRIX |
External reference:
| ID | Source |
|---|---|
| 4019574 | VUID |
| N0000147673 | NUI |
| D02841 | KEGG_DRUG |
| 153474 | RXNORM |
| C0019453 | UMLSCUI |
| CHEBI:24564 | CHEBI |
| CHEMBL1455 | ChEMBL_ID |
| DB00488 | DRUGBANK_ID |
| D006585 | MESH_DESCRIPTOR_UI |
| 2123 | PUBCHEM_CID |
| 7112 | IUPHAR_LIGAND_ID |
| 4825 | INN_ID |
| Q8BIH59O7H | UNII |
| 4156 | MMSL |
| 759 | MMSL |
| d01372 | MMSL |
| 387385000 | SNOMEDCT_US |
| 69879000 | SNOMEDCT_US |
| 4019574 | VANDF |
| 003567 | NDDF |
Pharmaceutical products:
None