OMACETAXINE MEPESUCCINATE HYDROCHLORIDE

US Previously Marketed

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C29H39NO9.ClH
Molecular Weight	582.082
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of OMACETAXINE MEPESUCCINATE HYDROCHLORIDE

Structure Search

SMILES

Cl.COC(=O)C[C@](O)(CCCC(C)(C)O)C(=O)O[C@H]1[C@H]2C3=CC4=C(OCO4)C=C3CCN5CCC[C@]25C=C1OC

InChI

InChIKey=RRNSZQVHVKGKOS-CALFFDBBSA-N

InChI=1S/C29H39NO9.ClH/c1-27(2,33)8-5-10-29(34,16-23(31)36-4)26(32)39-25-22(35-3)15-28-9-6-11-30(28)12-7-18-13-20-21(38-17-37-20)14-19(18)24(25)28;/h13-15,24-25,33-34H,5-12,16-17H2,1-4H3;1H/t24-,25-,28+,29-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C29H39NO9
Molecular Weight	545.6213
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	4 / 4
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23053254http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=23790799

Omacetaxine mepesuccinate (trade name Synribo) formerly named as homoharringtonine or HHT, is a pharmaceutical drug substance that is indicated for treatment of chronic myeloid leukemia (CML). It is a natural ester of the alkaloid cephalotaxine from Cephalotaxus harringtonia, now manufactured by hemi-synthesis. It was approved by the US FDA in October 2012 for the treatment of adult patients with CML with resistance and/or intolerance to two or more tyrosine kinase inhibitors (TKIs). The mechanism of action of omacetaxine mepesuccinate has not been fully elucidated but includes inhibition of protein synthesis and is independent of direct Bcr-Abl binding. Omacetaxine mepesuccinate binds to the A-site cleft in the peptidyl-transferase center of the large ribosomal subunit from a strain of archaeabacteria. In vitro, omacetaxine mepesuccinate reduced protein levels of the Bcr Abl oncoprotein and Mcl-1, an anti-apoptotic Bcl-2 family member. Omacetaxine mepesuccinate showed activity in mouse models of wild-type and T315I mutated Bcr-Abl CML.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
60S ribosomal protein L3 3 Target ID: P39023 Gene ID: 6122.0 Gene Symbol: RPL3 Target Organism: Homo sapiens (Human) Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	Antagonist 2849

Conditions

Condition	Modality	Highest Phase	Product
Chronic myeloid leukemia, chronic phase 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	Primary	Approved 8583	SYNRIBO Approved Use Indicated for the treatment of adult patients with chronic or accelerated phase chronic myeloid leukemia (CML) with resistance and/or intolerance to two or more tyrosine kinase inhibitors (TKI). This indication is based upon response rate.There are no trials verifying an improvement in disease-related symptoms or increased survival with SYNRIBO Launch Date 2012
Chronic myeloid leukemia, accelerated phase 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	Primary	Approved 8583	SYNRIBO Approved Use Indicated for the treatment of adult patients with chronic or accelerated phase chronic myeloid leukemia (CML) with resistance and/or intolerance to two or more tyrosine kinase inhibitors (TKI). This indication is based upon response rate.There are no trials verifying an improvement in disease-related symptoms or increased survival with SYNRIBO Launch Date 2012
Unknown 2596

C_max

Value	Dose	Analyte	Population
25.1 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3535355/	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
36.2 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3535355/	1.25 mg/m² 2 times / day multiple, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
28.6 ng/mL EXPERIMENT https://link.springer.com/article/10.1007/s10637-016-0360-9/tables/2	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
25.1 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23053254	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	[NO STEREO] OMACETAXINE MEPESUCCINATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
136.2 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3535355/	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
188 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3535355/	1.25 mg/m² 2 times / day multiple, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
188 ng × h/mL EXPERIMENT https://link.springer.com/article/10.1007/s10637-016-0360-9/tables/2	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
136.2 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23053254	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	[NO STEREO] OMACETAXINE MEPESUCCINATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
6.96 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3535355/	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7.03 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3535355/	1.25 mg/m² 2 times / day multiple, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.6 h EXPERIMENT https://link.springer.com/article/10.1007/s10637-016-0360-9/tables/2	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	OMACETAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.96 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23053254	1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered:	[NO STEREO] OMACETAXINE MEPESUCCINATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
50% REVIEW https://go.drugbank.com/drugs/DB04865	single, unknown		OMACETAXINE plasma	Homo sapiens population: age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
5 mg/m2 1 times / day multiple, subcutaneous MTD Dose: 5 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 5 mg/m2, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16847470	unhealthy, 57 years (range: 20–79 years) Health Status: unhealthy Age Group: 57 years (range: 20–79 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/16847470	DLT: Haematemesis, Pulmonary aspergillosis... Other AEs: Anasarca... Dose limiting toxicities: Haematemesis (grade 3, 1 patient) Pulmonary aspergillosis (grade 4, 1 patient) Skin rash (grade 3, 1 patient) Scalp pain (grade 3, 1 patient) Other AEs: Anasarca (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16847470
3 mg/m2 1 times / day multiple, subcutaneous Dose: 3 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 3 mg/m2, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16847470	unhealthy, 57 years (range: 20–79 years) Health Status: unhealthy Age Group: 57 years (range: 20–79 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/16847470	DLT: Hyperglycaemia, Diabetic hyperosmolar coma... Dose limiting toxicities: Hyperglycaemia (grade 3, 1 patient) Diabetic hyperosmolar coma Sources: https://pubmed.ncbi.nlm.nih.gov/16847470
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	unhealthy, 59 years Health Status: unhealthy Age Group: 59 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	Disc. AE: Thrombocytopenia, Alanine aminotransferase increased... Other AEs: Thrombocytopenia, Thrombocytopenia... AEs leading to discontinuation/dose reduction: Thrombocytopenia (2%) Alanine aminotransferase increased (2%) Other AEs: Thrombocytopenia (all grades, 74%) Thrombocytopenia (grade 3-4, 67%) Anemia (all grades, 61%) Anemia (grade 3-4, 36%) Neutropenia (all grades, 50%) Neutropenia (grade 3-4, 45%) Lymphopenia (all grades, 17%) Lymphopenia (grade 3-4, 16%) Bone marrow failure (all grades, 10%) Bone marrow failure (grade 3-4, 10%) Febrile neutropenia (all grades, 10%) Febrile neutropenia (grade 3-4, 10%) Diarrhea (all grades, 42%) Diarrhea (grade 3-4, 1%) Nausea (all grades, 32%) Nausea (grade 3-4, 1%) Constipation (grade 1-2, 15%) Abdominal pain upper (grade 1-2, 14%) Vomiting (grade 1-2, 12%) Fatigue (all grades, 26%) Fatigue (grade 3-4, 5%) Pyrexia (all grades, 24%) Pyrexia (grade 3-4, 1%) Asthenia (all grades, 23%) Asthenia (grade 3-4, 1%) Edema peripheral (grade 1-2, 13%) Infusion site reactions (grade 1-2, 34%) Arthralgia (all grades, 19%) Arthralgia (grade 3-4, 1%) Pain in extremity (all grades, 13%) Pain in extremity (grade 3-4, 1%) Back pain (all grades, 11%) Back pain (grade 3-4, 2%) Headache (all grades, 19%) Headache (grade 3-4, 1%) Insomnia (grade 1-2, 10%) Cough (all grades, 16%) Cough (grade 3-4, 1%) Epistaxis (all grades, 15%) Epistaxis (grade 3-4, 1%) Alopecia (grade 1-2, 15%) Rash (grade 1-2, 10%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf	unhealthy, 59 years Health Status: unhealthy Age Group: 59 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf	Disc. AE: Bone marrow failure, Sepsis... AEs leading to discontinuation/dose reduction: Bone marrow failure (1%) Sepsis (1%) Multiorgan failure (1%) Gout (1%) Renal failure (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	unhealthy, 59 years Health Status: unhealthy Age Group: 59 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	Other AEs: Anemia, Anemia... Other AEs: Anemia (all grades, 51%) Anemia (grade 3-4, 36%) Febrile neutropenia (all grades, 20%) Febrile neutropenia (grade 3-4, 16%) Neutropenia (all grades, 20%) Neutropenia (grade 3-4, 18%) Thrombocytopenia (all grades, 56%) Thrombocytopenia (grade 3-4, 49%) Diarrhea (all grades, 35%) Diarrhea (grade 3-4, 7%) Nausea (all grades, 27%) Nausea (grade 3-4, 4%) Vomiting (all grades, 15%) Vomiting (grade 3-4, 2%) Abdominal pain (grade 1-2, 13%) Fatigue (all grades, 31%) Fatigue (grade 3-4, 9%) Pyrexia (all grades, 29%) Pyrexia (grade 3-4, 2%) Asthenia (all grades, 24%) Asthenia (grade 3-4, 2%) Chills (grade 1-2, 13%) Infusion site reactions (grade 1-2, 22%) Anorexia (all grades, 13%) Anorexia (grade 3-4, 2%) Pain in extremity (all grades, 11%) Pain in extremity (grade 3-4, 2%) Headache (grade 1-2, 13%) Cough (grade 1-2, 15%) Dyspnea (all grades, 11%) Dyspnea (grade 3-4, 2%) Epistaxis (all grades, 11%) Epistaxis (grade 3-4, 2%) Bacterial infection (all grades, 56%) Bacterial infection (grade 3-4, 20%) Infection viral (all grades, 56%) Infection viral (grade 3-4, 20%) Fungal infection (all grades, 56%) Fungal infection (grade 3-4, 20%) Infection NOS (all grades, 56%) Infection NOS (grade 3-4, 20%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	unhealthy, 59 years Health Status: unhealthy Age Group: 59 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	Disc. AE: Alanine aminotransferase increased... AEs leading to discontinuation/dose reduction: Alanine aminotransferase increased (2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	unhealthy, 59 years Health Status: unhealthy Age Group: 59 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	Disc. AE: Pancytopenia... AEs leading to discontinuation/dose reduction: Pancytopenia (2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf	unhealthy, 59 years Health Status: unhealthy Age Group: 59 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf	Disc. AE: Tachyarrhythmia, Diplopia... AEs leading to discontinuation/dose reduction: Tachyarrhythmia (1%) Diplopia (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf
8 mg/m2 1 times / day multiple, intravenous Highest studied dose Dose: 8 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 8 mg/m2, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6478448	unhealthy Health Status: unhealthy Sources: https://pubmed.ncbi.nlm.nih.gov/6478448	DLT: Hypotension... Dose limiting toxicities: Hypotension Sources: https://pubmed.ncbi.nlm.nih.gov/6478448
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf	Disc. AE: Gastrointestinal disorders, Gingival hemorrhage... AEs leading to discontinuation/dose reduction: Gastrointestinal disorders (1 patient) Gingival hemorrhage (1 patient) Alopecia (1 patient) Thrombocytopenia (grade 4, 1 patient) Neutropenia (grade 4, 1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf	Disc. AE: Gingival hemorrhage, Gastrointestinal disorders... AEs leading to discontinuation/dose reduction: Gingival hemorrhage (1 patient) Gastrointestinal disorders (1 patient) Alopecia (1 patient) Thrombocytopenia (grade 4, 1 patient) Neutropenia (grade 4, 1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000MedR.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252		inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A 70 CYP2C19 2057 P-gp 1741	CYP 303 P-gp 2052	CYP1A 59

Drug as perpetrator

Target	Modality	Activity	Metabolite
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000ClinPharmR.pdf#page=20 Page: 20.0	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61,56	strong [Inhibition 10 uM]
CYP1A 122	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61,56	weak [Inhibition 10 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61,56	weak [Inhibition 10 uM]	DMHHT 3
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61,56	weak [Inhibition 10 uM]
CYP1A 122	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61.0	weak

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP 303	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=54 Page: 54.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000ClinPharmR.pdf#page=20 Page: 20.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=43 Page: 43.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA00BBK4	https://www.aablocks.com/goods/Goods/detail?id=AA00BBK4
Aaron Chemicals	AR00BCBW	http://www.aaronchem.com/24316-19-6
abcr GmbH	AB479786	http://www.abcr.com/shop/en/AB479786
AbMole Bioscience	M3942	http://www.abmole.com/products/cephalotaxine.html
Achemtek	0104-028087	http://www.achemtek.com/24316-19-6
Acorn PharmaTech	ACN-035228	http://www.acornpharmatech.com/
AHH Chemical co.,ltd	NP-0431	http://www.ahhchemical.com/product/NP-0431.html
Ambeed	A863555	https://www.ambeed.com/products/24316-19-6.html
Angene	AGN-PC-0R05OB	http://www.angenechemical.com/productshow/AGN-PC-0R05OB.html
Aurum Pharmatech LLC	S-7655	http://www.Aurumpharmatech.com/Product/ProductDetails/S_7655
AvaChem Scientific	3156	http://www.avachem.com/productSearch.asp?3156
BLD Pharm	BD16925	http://www.bldpharm.com/products/24316-19-6.html
Chem Scene	CS-3006	http://www.chemscene.com/24316-19-6.html
ChemFaces	CFN90919	http://www.chemfaces.com/natural/Cephalotaxine-CFN90919.html
Chemspace	CSSB00000036076	https://chem-space.com/CSSB00000036076
CSNpharm	CSN12450	https://www.csnpharm.com/products/cephalotaxine.html
DC Chemicals	DC9649	http://www.dcchemicals.com/product_show-Cephalotaxlen.html
eNovation Chemicals	D574859	http://www.enovationchem.com/productDetails.asp?productID=D574859
eNovation Chemicals	D628756	https://www.enovationchem.com/ProductDetails.asp?ProductID=D628756
eNovation Chemicals	D679660	https://www.enovationchem.com/ProductDetails.asp?ProductID=D679660
Hairui	HR120093	http://www.hairuichem.com/en/product/24316-19-6.html
Lab Network	LN00176704	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00176704
Matrix Scientific	76038	https://www.matrixscientific.com/076038.html
MedChem Express	HY-N0838	https://www.medchemexpress.com/cephalotaxlen.html
MuseChem	I002813	https://www.musechem.com/product/I002813.html
Oakwood	79392	http://www.oakwoodchemical.com/p-73475-079392.aspx
Smolecule	S523194	http://www.smolecule.com/products/s523194
Smolecule	S749414	https://www.smolecule.com/products/s749414
THE BioTek	bt-263600	https://www.thebiotek.com/product/inhibitors/bt-263600

PubMed

Title	Date	PubMed
Activity of drugs from traditional Chinese medicine toward sensitive and MDR1- or MRP1-overexpressing multidrug-resistant human CCRF-CEM leukemia cells.	2002 Mar-Apr	12064912

Patents

Sample Use Guides

In Vivo Use Guide

Unknown

Route of Administration: Unknown

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:11:52 GMT 2025` Edited by `admin` on `Mon Mar 31 18:11:52 GMT 2025`
Record UNII	563OX5661H
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

OMACETAXINE MEPESUCCINATE HYDROCHLORIDE

Common Name

English

CEPHALOTAXINE, 4-METHYL (2R)-2-HYDROXY-2-(4-HYDROXY-4-METHYLPENTYL)BUTANEDIOATE (ESTER), HYDROCHLORIDE

Preferred Name

English

Code System Code Type Description

CAS

457895-79-3

Created by admin on Mon Mar 31 18:11:52 GMT 2025 , Edited by admin on Mon Mar 31 18:11:52 GMT 2025

PRIMARY

PUBCHEM

9851264

Created by admin on Mon Mar 31 18:11:52 GMT 2025 , Edited by admin on Mon Mar 31 18:11:52 GMT 2025

PRIMARY

DRUG BANK

DBSALT001930

Created by admin on Mon Mar 31 18:11:52 GMT 2025 , Edited by admin on Mon Mar 31 18:11:52 GMT 2025

PRIMARY

FDA UNII

563OX5661H

Created by admin on Mon Mar 31 18:11:52 GMT 2025 , Edited by admin on Mon Mar 31 18:11:52 GMT 2025

PRIMARY

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SMILES

InChI

DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23053254http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdfCurator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=23790799

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23053254http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=23790799

C_max

T_1/2

F_unbound

Drug as perpetrator