Details of the Drug

General Information of Drug (ID: DMPU2WX)

Drug Name

Omacetaxine mepesuccinate

Synonyms

Synribo (TN)

Indication

Disease Entry	ICD 11	Status	REF
Chronic myeloid leukaemia	2A20	Approved	[1], [2]

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 2

Molecular Weight (mw)

545.6

Topological Polar Surface Area (xlogp)

0.8

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Clearance: The drug present in the plasma can be removed from the body at the rate of 2.96 mL/min/kg [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 6 hours [3]
Metabolism: The drug is metabolized via the hepatic [4]
Vd: The volume of distribution (Vd) of drug is 141 +/- 93.4 L [5]

Chemical Identifiers

Formula: C29H39NO9
IUPAC Name: 1-O-[(2S,3S,6R)-4-methoxy-16,18-dioxa-10-azapentacyclo[11.7.0.02,6.06,10.015,19]icosa-1(20),4,13,15(19)-tetraen-3-yl] 4-O-methyl (2R)-2-hydroxy-2-(4-hydroxy-4-methylpentyl)butanedioate
Canonical SMILES: CC(C)(CCC[C@@](CC(=O)OC)(C(=O)O[C@H]1[C@H]2C3=CC4=C(C=C3CCN5[C@@]2(CCC5)C=C1OC)OCO4)O)O
InChI: InChI=1S/C29H39NO9/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/t24-,25-,28+,29-/m1/s1
InChIKey: HYFHYPWGAURHIV-JFIAXGOJSA-N

Cross-matching ID

PubChem CID: 285033
ChEBI ID: CHEBI:71019
CAS Number: 26833-87-4
DrugBank ID: DB04865
TTD ID: D0M4XY
ACDINA ID: D01298

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Ribosome A (hRA)	TTA4FIU	NOUNIPROTAC	Modulator	[6]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Omacetaxine mepesuccinate

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Fedratinib	DM4ZBK6	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Fedratinib.	Myeloproliferative neoplasm [2A20]	[8]
Nilotinib	DM7HXWT	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Nilotinib.	Myeloproliferative neoplasm [2A20]	[9]
Ruxolitinib	DM7Q98D	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Ruxolitinib.	Myeloproliferative neoplasm [2A20]	[8]
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Coadministration of a Drug Treating the Disease Different from Omacetaxine mepesuccinate (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Midostaurin	DMI6E0R	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Midostaurin.	Acute myeloid leukaemia [2A60]	[9]
Inotersen	DMJ93CT	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Inotersen.	Amyloidosis [5D00]	[8]
Siltuximab	DMGEATB	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Siltuximab.	Anemia [3A00-3A9Z]	[9]
Dupilumab	DMOAD2Y	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Dupilumab.	Atopic eczema [EA80]	[9]
Eribulin	DM1DX4Q	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Eribulin.	Breast cancer [2C60-2C6Y]	[9]
Talazoparib	DM1KS78	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Talazoparib.	Breast cancer [2C60-2C6Y]	[9]
LY2835219	DM93VBZ	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and LY2835219.	Breast cancer [2C60-2C6Y]	[9]
Pralatrexate	DMAO80I	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Pralatrexate.	Breast cancer [2C60-2C6Y]	[9]
Palbociclib	DMD7L94	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Palbociclib.	Breast cancer [2C60-2C6Y]	[9]
Cabazitaxel	DMPAZHC	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Cabazitaxel.	Breast cancer [2C60-2C6Y]	[9]
Bosutinib	DMTI8YE	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Bosutinib.	Breast cancer [2C60-2C6Y]	[9]
Regorafenib	DMHSY1I	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Regorafenib.	Colorectal cancer [2B91]	[8]
Aflibercept	DMT3D5I	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Aflibercept.	Colorectal cancer [2B91]	[9]
Ardeparin	DMYRX8B	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Ardeparin.	Coronary thrombosis [BA43]	[8]
Danaparoid	DM6CLBN	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Danaparoid.	Deep vein thrombosis [BD71]	[8]
Rivaroxaban	DMQMBZ1	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Rivaroxaban.	Deep vein thrombosis [BD71]	[8]
Polatuzumab vedotin	DMF6Y0L	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Polatuzumab vedotin.	Diffuse large B-cell lymphoma [2A81]	[9]
Lisocabtagene maraleucel	DMP45ME	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Lisocabtagene maraleucel.	Diffuse large B-cell lymphoma [2A81]	[9]
Axicabtagene ciloleucel	DMYHN59	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Axicabtagene ciloleucel.	Diffuse large B-cell lymphoma [2A81]	[9]
Bay 80-6946	DMLOS5R	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Bay 80-6946.	Follicular lymphoma [2A80]	[9]
Tazemetostat	DMWP1BH	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Tazemetostat.	Follicular lymphoma [2A80]	[8]
Avapritinib	DMK2GZX	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Avapritinib.	Gastrointestinal stromal tumour [2B5B]	[8]
177Lu-DOTATATE	DMT8GVU	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and 177Lu-DOTATATE.	Hepatitis virus infection [1E50-1E51]	[9]
Brentuximab vedotin	DMWLC57	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Brentuximab vedotin.	Hodgkin lymphoma [2B30]	[9]
Teriflunomide	DMQ2FKJ	Major	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[10]
Olaratumab	DMNYOIX	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Olaratumab.	Kaposi sarcoma [2B57]	[9]
Denosumab	DMNI0KO	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Denosumab.	Low bone mass disorder [FB83]	[11]
Brigatinib	DM7W94S	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Brigatinib.	Lung cancer [2C25]	[9]
Lurbinectedin	DMEFRTZ	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Lurbinectedin.	Lung cancer [2C25]	[9]
Osimertinib	DMRJLAT	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Osimertinib.	Lung cancer [2C25]	[9]
Belimumab	DM3OBQF	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Belimumab.	Lupus erythematosus [4A40]	[9]
Inotuzumab ozogamicin	DMAC130	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Inotuzumab ozogamicin.	Malignant haematopoietic neoplasm [2B33]	[9]
Ofatumumab	DM295PR	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Ofatumumab.	Mature B-cell leukaemia [2A82]	[9]
Obinutuzumab	DM3BVAE	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Obinutuzumab.	Mature B-cell leukaemia [2A82]	[9]
GDC-0199	DMH0QKA	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and GDC-0199.	Mature B-cell leukaemia [2A82]	[9]
IPI-145	DMWA24P	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and IPI-145.	Mature B-cell leukaemia [2A82]	[9]
Acalabrutinib	DM7GCVW	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Acalabrutinib.	Mature B-cell lymphoma [2A85]	[8]
Blinatumomab	DMGECIJ	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Blinatumomab.	Mature B-cell lymphoma [2A85]	[9]
Ibrutinib	DMHZCPO	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Ibrutinib.	Mature B-cell lymphoma [2A85]	[9]
Ponatinib	DMYGJQO	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Ponatinib.	Mature B-cell lymphoma [2A85]	[9]
Arry-162	DM1P6FR	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Arry-162.	Melanoma [2C30]	[8]
Ipilimumab	DMJTIYK	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Ipilimumab.	Melanoma [2C30]	[9]
LGX818	DMNQXV8	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and LGX818.	Melanoma [2C30]	[8]
Carfilzomib	DM48K0X	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Carfilzomib.	Multiple myeloma [2A83]	[9]
Selinexor	DMBD4K3	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Selinexor.	Multiple myeloma [2A83]	[9]
Belantamab mafodotin	DMBT3AI	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Belantamab mafodotin.	Multiple myeloma [2A83]	[9]
Elotuzumab	DMEYHG9	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Elotuzumab.	Multiple myeloma [2A83]	[9]
Daratumumab	DMKCIUZ	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Daratumumab.	Multiple myeloma [2A83]	[9]
Tecfidera	DM2OVDT	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Tecfidera.	Multiple sclerosis [8A40]	[9]
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Siponimod.	Multiple sclerosis [8A40]	[12]
Fingolimod	DM5JVAN	Major	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Fingolimod.	Multiple sclerosis [8A40]	[13]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Ocrelizumab.	Multiple sclerosis [8A40]	[9]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Ozanimod.	Multiple sclerosis [8A40]	[14]
Deflazacort	DMV0RNS	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Deflazacort.	Muscular dystrophy [8C70]	[9]
Romidepsin	DMT5GNL	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Romidepsin.	Mycosis fungoides [2B01]	[9]
Prasugrel	DM7MT6E	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Prasugrel.	Myocardial infarction [BA41-BA43]	[8]
Inebilizumab	DMI0RHA	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Inebilizumab.	Nervous system paraneoplastic/autoimmune disorder [8E4A]	[9]
Atezolizumab	DMMF8U0	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Atezolizumab.	Non-small cell lung cancer [2C25]	[9]
Olaparib	DM8QB1D	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Olaparib.	Ovarian cancer [2C73]	[9]
Rucaparib	DM9PVX8	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Rucaparib.	Ovarian cancer [2C73]	[9]
MK-4827	DMLYGH4	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and MK-4827.	Ovarian cancer [2C73]	[9]
Brodalumab	DMASDQ6	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Brodalumab.	Psoriasis [EA90]	[9]
Ustekinumab	DMHTYK3	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Ustekinumab.	Psoriasis [EA90]	[9]
Tildrakizumab	DMLW9HG	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Tildrakizumab.	Psoriasis [EA90]	[9]
Risankizumab	DMM32GT	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Risankizumab.	Psoriasis [EA90]	[9]
Ixekizumab	DMXW92T	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Ixekizumab.	Psoriasis [EA90]	[9]
Temsirolimus	DMS104F	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Temsirolimus.	Renal cell carcinoma [2C90]	[9]
Tocilizumab	DM7J6OR	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Tocilizumab.	Rheumatoid arthritis [FA20]	[9]
Canakinumab	DM8HLO5	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Canakinumab.	Rheumatoid arthritis [FA20]	[15]
Rilonacept	DMGLUQS	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Rilonacept.	Rheumatoid arthritis [FA20]	[15]
Golimumab	DMHZV7X	Major	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Golimumab.	Rheumatoid arthritis [FA20]	[16]
Sarilumab	DMOGNXY	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Sarilumab.	Rheumatoid arthritis [FA20]	[9]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Omacetaxine mepesuccinate when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[17]
Mogamulizumab	DMISH0Z	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Mogamulizumab.	Sezary syndrome [2B02]	[9]
PDX-101	DM6OC53	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and PDX-101.	Solid tumour/cancer [2A00-2F9Z]	[9]
Trabectedin	DMG3Y89	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Trabectedin.	Solid tumour/cancer [2A00-2F9Z]	[9]
LEE011	DMMX75K	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and LEE011.	Solid tumour/cancer [2A00-2F9Z]	[9]
Triptorelin	DMTK4LS	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Triptorelin.	Solid tumour/cancer [2A00-2F9Z]	[9]
Pomalidomide	DMTGBAX	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Pomalidomide.	Systemic sclerosis [4A42]	[9]
Plicamycin	DM7C8YV	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Plicamycin.	Testicular cancer [2C80]	[8]
Caplacizumab	DMPUKA7	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Caplacizumab.	Thrombocytopenia [3B64]	[8]
Apixaban	DM89JLN	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Apixaban.	Thrombosis [DB61-GB90]	[8]
Cangrelor	DM8JRH0	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Cangrelor.	Thrombosis [DB61-GB90]	[8]
Brilinta	DMBR01X	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Brilinta.	Thrombosis [DB61-GB90]	[8]
Cabozantinib	DMIYDT4	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Cabozantinib.	Thyroid cancer [2D10]	[18]
Belatacept	DMXLYQF	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Belatacept.	Transplant rejection [NE84]	[9]
Durvalumab	DM4PVDY	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Durvalumab.	Ureteral cancer [2C92]	[9]
Fluticasone	DMGCSVF	Moderate	Additive immunosuppressive effects by the combination of Omacetaxine mepesuccinate and Fluticasone.	Vasomotor/allergic rhinitis [CA08]	[9]
Betrixaban	DM2C4RF	Major	Increased risk of bleeding by the combination of Omacetaxine mepesuccinate and Betrixaban.	Venous thromboembolism [BD72]	[8]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Omacetaxine Mepesuccinate 3.5mg/vial powder	3.5mg/vial	Powder	Subcutaneous

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7454).
2	Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
3	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
4	FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
5	An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
6	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
7	Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
8	Product Information. Brukinsa (zanubrutinib). BeiGene USA, Inc, San Mateo, CA.
9	Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
10	Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
11	Product Information. Lonsurf (tipiracil-trifluridine). Taiho Oncology, Inc., Princeton, NJ.
12	Cerner Multum, Inc. "Australian Product Information.".
13	Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
14	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
15	Product Information. Arcalyst (rilonacept). Regeneron Pharmaceuticals Inc, Tarrytown, NY.
16	Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
17	CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]
18	Bodiford AB, Kessler FO, Fermo JD, Ragucci KR "Elevated international normalized ratio with the consumption of grapefruit and use of warfarin." SAGE Open Med Case Rep 0 (2013): 1-3. [PMID: 27489634]