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

Stem definition	Drug id	CAS RN
	4677	26833-87-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: omacetaxine mepesuccinate synribo homoharringtonine CGX-635 NSC 141633 NSC-141633	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. Molecular weight: 545.63 Formula: C29H39NO9 CLOGP: 1.76 LIPINSKI: 1 HAC: 10 HDO: 2 TPSA: 123.99 ALOGS: -3.70 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

omacetaxine mepesuccinate
synribo
homoharringtonine
CGX-635
NSC 141633
NSC-141633

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.

Molecular weight: 545.63
Formula: C29H39NO9
CLOGP: 1.76
LIPINSKI: 1
HAC: 10
HDO: 2
TPSA: 123.99
ALOGS: -3.70
ROTB: 11

Status: OFP

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

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
Bone marrow failure	66.15	44.45	20	490	27604	50577010
Platelet count decreased	53.46	44.45	24	486	100702	50503912
Injection site erythema	49.99	44.45	21	489	74915	50529699

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
Injection site erythema	57.62	45.20	17	444	13939	29560127
Platelet count decreased	45.47	45.20	25	436	104647	29469419

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
Bone marrow failure	76.29	38.04	27	796	47925	64449984
Platelet count decreased	74.25	38.04	38	785	167673	64330236
Injection site erythema	55.94	38.04	24	799	70776	64427133
Nausea	44.72	38.04	52	771	785748	63712161

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 agents
CHEBI has role	CHEBI:48001	protein synthesis inhibitors
CHEBI has role	CHEBI:68495	Type I cell-death inducers
CHEBI has role	CHEBI:149553	anticoronaviral drug

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	RX	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
24316-19-6	SECONDARY_CAS_RN
DB04865	DRUGBANK_ID
6FG8041S5B	UNII
285033	PUBCHEM_CID
65305	PUBCHEM_CID
1356689	RXNORM
194347	MMSL
27023	MMSL
d07573	MMSL
009753	NDDF
421021001	SNOMEDCT_US
421815001	SNOMEDCT_US
D000077863	MESH_DESCRIPTOR_UI
C0062941	UMLSCUI
C3528000	UMLSCUI
84MI6OYN4Z	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
SYNRIBO	HUMAN PRESCRIPTION DRUG LABEL	1	63459-177	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	3.50 mg	SUBCUTANEOUS	NDA	27 sections