omacetaxine mepesuccinate 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: 2.33 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	63.96	44.74	20	470	29649	46655923
Platelet count decreased	52.70	44.74	24	466	100000	46585572
Injection site erythema	49.33	44.74	21	469	74406	46611166

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	58.28	40.90	17	436	13817	29938208
Platelet count decreased	45.86	40.90	25	428	106104	29845921
Blood count abnormal	43.27	40.90	13	440	11639	29940386

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	cytostatic
CHEBI has role	CHEBI:48001	protein synthesis inhibitors
CHEBI has role	CHEBI:68495	type i programmed cell-death inducer
CHEBI has role	CHEBI:149553	anti-coronaviral agents

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Chronic myeloid leukemia	indication	92818009	DOID:8552

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)

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
SARS-CoV-2	Virus			INHIBITOR	EC50	5.59		SCIENTIFIC LITERATURE

External reference:

ID	Source
D08956	KEGG_DRUG
4031782	VUID
N0000186058	NUI
24316-19-6	SECONDARY_CAS_RN
4031782	VANDF
4031814	VANDF
C2709279	UMLSCUI
C3528000	UMLSCUI
CHEBI:71019	CHEBI
HMT	PDB_CHEM_ID
CHEMBL46286	ChEMBL_ID
DB04865	DRUGBANK_ID
D000077863	MESH_DESCRIPTOR_UI
285033	PUBCHEM_CID
7454	IUPHAR_LIGAND_ID
8885	INN_ID
6FG8041S5B	UNII
84MI6OYN4Z	UNII
65305	PUBCHEM_CID
1356689	RXNORM
194347	MMSL
27023	MMSL
d07573	MMSL
009753	NDDF
421021001	SNOMEDCT_US
421815001	SNOMEDCT_US

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