ixabepilone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1517 | 219989-84-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Ixabepilone is a semi-synthetic analog of epothilone B. Ixabepilone binds directly to beta-tubulin subunits on microtubules, leading to suppression of microtubule dynamics. Ixabepilone suppresses the dynamic instability of alphaBeta-II and alphaBeta-III microtubules. Ixabepilone possesses low in vitro susceptibility to multiple tumor resistance mechanisms including efflux transporters, such as MRP-1 and P-glycoprotein (P-gp). Ixabepilone blocks cells in the mitotic phase of the cell division cycle, leading to cell death.
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) | 5.60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.97 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 11 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.20 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 17 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 16, 2007 | FDA | BRISTOL MYERS SQUIBB |
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 |
|---|---|---|---|---|---|---|
| Pseudocirrhosis | 189.37 | 37.69 | 30 | 1784 | 677 | 63486531 |
| Neutrophil count decreased | 127.47 | 37.69 | 51 | 1763 | 56355 | 63430853 |
| Portal hypertension | 94.98 | 37.69 | 22 | 1792 | 3797 | 63483411 |
| White blood cell count decreased | 83.74 | 37.69 | 51 | 1763 | 139053 | 63348155 |
| Anaemia | 73.28 | 37.69 | 63 | 1751 | 293367 | 63193841 |
| Neutropenia | 66.08 | 37.69 | 48 | 1766 | 174957 | 63312251 |
| Febrile neutropenia | 48.09 | 37.69 | 34 | 1780 | 118415 | 63368793 |
| Platelet count decreased | 46.37 | 37.69 | 33 | 1781 | 116089 | 63371119 |
| Malignant neoplasm progression | 43.95 | 37.69 | 28 | 1786 | 82093 | 63405115 |
| Dehydration | 42.64 | 37.69 | 37 | 1777 | 173317 | 63313891 |
| Disease progression | 42.48 | 37.69 | 32 | 1782 | 122726 | 63364482 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Pseudocirrhosis | 188.63 | 36.74 | 28 | 1420 | 652 | 79742288 |
| Neutrophil count decreased | 124.83 | 36.74 | 51 | 1397 | 93908 | 79649032 |
| White blood cell count decreased | 99.34 | 36.74 | 54 | 1394 | 188234 | 79554706 |
| Portal hypertension | 86.21 | 36.74 | 21 | 1427 | 7087 | 79735853 |
| Anaemia | 65.27 | 36.74 | 58 | 1390 | 444957 | 79297983 |
| Neutropenia | 49.14 | 36.74 | 41 | 1407 | 287669 | 79455271 |
| Platelet count decreased | 44.56 | 36.74 | 33 | 1415 | 194631 | 79548309 |
| Febrile neutropenia | 39.55 | 36.74 | 33 | 1415 | 230966 | 79511974 |
| Malignant neoplasm progression | 37.87 | 36.74 | 26 | 1422 | 135964 | 79606976 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01DC04 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS CYTOTOXIC ANTIBIOTICS AND RELATED SUBSTANCES Other cytotoxic antibiotics |
| FDA PE | N0000175085 | Microtubule Inhibition |
| FDA EPC | N0000175592 | Microtubule Inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:61951 | microtubule destabilizing role |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Carcinoma of breast | indication | 254838004 | DOID:3459 |
| Metastatic Breast Carcinoma | indication | ||
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Hepatic failure | contraindication | 59927004 | |
| Acute infectious disease | contraindication | 63171007 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Liver function tests abnormal | contraindication | 166603001 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Peripheral nerve disease | contraindication | 302226006 | |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.56 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 15MG/VIAL | IXEMPRA KIT | R-PHARM US LLC | N022065 | Oct. 16, 2007 | RX | INJECTABLE | INTRAVENOUS | 7312237 | Aug. 21, 2024 | USE OF IXABEPILONE IN COMBINATION WITH CAPECITABINE IN TREATMENT OF METASTASIS BREAST CANCER |
| 45MG/VIAL | IXEMPRA KIT | R-PHARM US LLC | N022065 | Oct. 16, 2007 | RX | INJECTABLE | INTRAVENOUS | 7312237 | Aug. 21, 2024 | USE OF IXABEPILONE IN COMBINATION WITH CAPECITABINE IN TREATMENT OF METASTASIS BREAST CANCER |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Tubulin beta | Tumour-associated antigen | INHIBITOR | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||||
| Apoptosis regulator Bcl-2 | Cytosolic other | Kd | 6.47 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4026737 | VUID |
| N0000179767 | NUI |
| D04645 | KEGG_DRUG |
| 4026737 | VANDF |
| C1135132 | UMLSCUI |
| CHEBI:63605 | CHEBI |
| GZX | PDB_CHEM_ID |
| CHEMBL1201752 | ChEMBL_ID |
| DB04845 | DRUGBANK_ID |
| C430592 | MESH_SUPPLEMENTAL_RECORD_UI |
| 6824 | IUPHAR_LIGAND_ID |
| 8390 | INN_ID |
| K27005NP0A | UNII |
| 6445540 | PUBCHEM_CID |
| 337523 | RXNORM |
| 121505 | MMSL |
| 24628 | MMSL |
| d07051 | MMSL |
| 012371 | NDDF |
| 428282007 | SNOMEDCT_US |
| 429022006 | SNOMEDCT_US |
Pharmaceutical products:
None