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omacetaxine mepesuccinate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4677 | 26833-87-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Semisynthetic derivative of harringtonine that acts as a protein synthesis inhibitor and induces APOPTOSIS in tumor cells. It is used in the treatment of MYELOID LEUKEMIA, CHRONIC.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 1.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.96 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 9.80 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PRKDC,SYK,TEK,TGFBR1,ZAP70 | 26 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 26, 2012 | FDA | IVAX INTL |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 387.09 | 50.52 | 90 | 718 | 53501 | 90574138 |
| Platelet count decreased | 94.71 | 50.52 | 38 | 770 | 136931 | 90490708 |
| Bone marrow failure | 61.15 | 50.52 | 19 | 789 | 32202 | 90595437 |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 457.47 | 51.39 | 115 | 783 | 40346 | 42580091 |
| Platelet count decreased | 68.39 | 51.39 | 40 | 858 | 138541 | 42481896 |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 826.15 | 48.38 | 202 | 1367 | 94138 | 110493592 |
| Platelet count decreased | 143.00 | 48.38 | 68 | 1501 | 230375 | 110357355 |
| Granulocyte count decreased | 68.88 | 48.38 | 15 | 1554 | 3959 | 110583771 |
| Bone marrow failure | 68.36 | 48.38 | 27 | 1542 | 57821 | 110529909 |
| Nausea | 66.59 | 48.38 | 84 | 1485 | 1235606 | 109352124 |
| White blood cell count decreased | 66.59 | 48.38 | 41 | 1528 | 229349 | 110358381 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XX40 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D000972 | Antineoplastic Agents, Phytogenic |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D011500 | Protein Synthesis Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:48001 | protein synthesis inhibitor |
| CHEBI has role | CHEBI:68495 | apoptosis inducer |
| CHEBI has role | CHEBI:149553 | anticoronaviral agent |
Related Drugs by ATC class:
L01XX Other antineoplastic agents 33 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic myeloid leukemia | indication | 92818009 | DOID:8552 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.86 | acidic |
| pKa2 | 8.15 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 3.5MG/VIAL | SYNRIBO | TEVA PHARMS INTL | N203585 | Oct. 26, 2012 | DISCN | POWDER | SUBCUTANEOUS | 6987103 | Oct. 26, 2026 | TREATMENT OF PATIENTS WITH TYROSINE KINASE INHIBITOR (TKI) RESISTANT OR INTOLERANT CHRONIC MYELOID/MYELOGENOUS LEUKEMIA (CML) |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D08956 | KEGG_DRUG |
| 4031782 | VUID |
| N0000186058 | NUI |
| 4031782 | VANDF |
| 4031814 | VANDF |
| CHEBI:71019 | CHEBI |
| HMT | PDB_CHEM_ID |
| CHEMBL46286 | ChEMBL_ID |
| 7454 | IUPHAR_LIGAND_ID |
| 8885 | INN_ID |
| DB04865 | DRUGBANK_ID |
| 6FG8041S5B | UNII |
| 1356689 | RXNORM |
| 194347 | MMSL |
| 27023 | MMSL |
| d07573 | MMSL |
| 009753 | NDDF |
| 421021001 | SNOMEDCT_US |
| 421815001 | SNOMEDCT_US |
| C0062941 | UMLSCUI |
| C3528000 | UMLSCUI |
| D000077863 | MESH_DESCRIPTOR_UI |
| 285033 | PUBCHEM_CID |
| 24316-19-6 | SECONDARY_CAS_RN |
| 65305 | PUBCHEM_CID |
| 84MI6OYN4Z | UNII |
| 6FG8041S5B | INXIGHT DRUGS |
| 84MI6OYN4Z | INXIGHT DRUGS |
Pharmaceutical products:
None