Details of the Drug

General Information of Drug (ID: DMU1LXS)

Drug Name
Trastuzumab emtansine
Indication
Disease Entry ICD 11 Status REF
HER2-positive breast cancer 2C60-2C65 Phase 3 [1]
Breast cancer 2C60-2C65 Phase 2 [1]
Drug Type
Antibody drug conjugate
ADMET Property
Half-life
The concentration or amount of drug in body reduced by one-half in 4 days [2]
Vd
The volume of distribution (Vd) of drug is 3.13 L []
Cross-matching ID
PubChem CID
166596981
DrugBank ID
DB05773
TTD ID
D0UG0K
INTEDE ID
DR1629

Molecular Interaction Atlas of This Drug


Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [3]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [4]
Aldo-keto reductase 1C3 (AKR1C3) DEGQTXO AK1C3_HUMAN Substrate [5]
Aldo-keto reductase 1C1 (AKR1C1) DE7P2FB AK1C1_HUMAN Substrate [5]
Aldo-keto reductase 1C2 (AKR1C2) DEOY5ZM AK1C2_HUMAN Substrate [5]
Aldo-keto reductase 1C4 (AKR1C4) DEAJN47 AK1C4_HUMAN Substrate [5]
NADPH-dependent carbonyl reductase 3 (CBR3) DEIVKZ8 CBR3_HUMAN Substrate [5]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Gene/Protein Processing [6]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Gene/Protein Processing [6]
Receptor tyrosine-protein kinase erbB-2 (ERBB2) OTOAUNCK ERBB2_HUMAN Protein Interaction/Cellular Processes [7]
Molecular Interaction Atlas (MIA) 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 Trastuzumab emtansine
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Tucatinib DMBESUA Moderate Decreased metabolism of Trastuzumab Emtansine caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [8]
Coadministration of a Drug Treating the Disease Different from Trastuzumab emtansine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [9]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [10]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Trastuzumab Emtansine caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [8]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [11]
Levomilnacipran DMV26S8 Moderate Increased risk of bleeding by the combination of Trastuzumab Emtansine and Levomilnacipran. Chronic pain [MG30] [12]
Regorafenib DMHSY1I Major Increased risk of bleeding by the combination of Trastuzumab Emtansine and Regorafenib. Colorectal cancer [2B91] [13]
Vilazodone DM4LECQ Moderate Increased risk of bleeding by the combination of Trastuzumab Emtansine and Vilazodone. Depression [6A70-6A7Z] [12]
Vortioxetine DM6F1PU Moderate Increased risk of bleeding by the combination of Trastuzumab Emtansine and Vortioxetine. Depression [6A70-6A7Z] [12]
Cenobamate DM8KLU9 Moderate Increased metabolism of Trastuzumab Emtansine caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [14]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and Cannabidiol. Epileptic encephalopathy [8A62] [13]
Avapritinib DMK2GZX Major Increased risk of bleeding by the combination of Trastuzumab Emtansine and Avapritinib. Gastrointestinal stromal tumour [2B5B] [13]
Boceprevir DMBSHMF Moderate Decreased metabolism of Trastuzumab Emtansine caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [8]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and Brentuximab vedotin. Hodgkin lymphoma [2B30] [15]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Trastuzumab Emtansine caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [8]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and Teriflunomide. Hyper-lipoproteinaemia [5C80] [16]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and BMS-201038. Hyper-lipoproteinaemia [5C80] [17]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [18]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Trastuzumab Emtansine and Idelalisib. Mature B-cell leukaemia [2A82] [19]
Acalabrutinib DM7GCVW Major Increased risk of bleeding by the combination of Trastuzumab Emtansine and Acalabrutinib. Mature B-cell lymphoma [2A85] [20]
Ibrutinib DMHZCPO Major Increased risk of bleeding by the combination of Trastuzumab Emtansine and Ibrutinib. Mature B-cell lymphoma [2A85] [21]
Ponatinib DMYGJQO Major Increased risk of bleeding by the combination of Trastuzumab Emtansine and Ponatinib. Mature B-cell lymphoma [2A85] [20]
Panobinostat DM58WKG Major Increased risk of bleeding by the combination of Trastuzumab Emtansine and Panobinostat. Multiple myeloma [2A83] [8]
Nepafenac DMYK490 Moderate Increased risk of bleeding by the combination of Trastuzumab Emtansine and Nepafenac. Osteoarthritis [FA00-FA05] [22]
MK-4827 DMLYGH4 Moderate Increased risk of bleeding by the combination of Trastuzumab Emtansine and MK-4827. Ovarian cancer [2C73] [13]
Abametapir DM2RX0I Moderate Decreased metabolism of Trastuzumab Emtansine caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [23]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Trastuzumab Emtansine caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [8]
Larotrectinib DM26CQR Moderate Decreased metabolism of Trastuzumab Emtansine caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [8]
Cabozantinib DMIYDT4 Major Increased risk of bleeding by the combination of Trastuzumab Emtansine and Cabozantinib. Thyroid cancer [2D10] [24]
⏷ Show the Full List of 28 DDI Information of This Drug

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
3 Drug-Drug interactions of clinical significance in the treatment of patients with Mycobacterium avium complex disease. Clin Pharmacokinet. 2000 Sep;39(3):203-14.
4 Trastuzumab emtansine. An inadequately assessed combination of two cytotoxic drugs. Prescrire Int. 2014 Dec;23(155):289.
5 The role of carbonyl reducing enzymes in oxcarbazepine in vitro metabolism in man. Chem Biol Interact. 2014 Sep 5;220:241-7.
6 CDK4/6 inhibition provides a potent adjunct to Her2-targeted therapies in preclinical breast cancer models. Genes Cancer. 2014 Jul;5(7-8):261-72. doi: 10.18632/genesandcancer.24.
7 Preclinical safety profile of trastuzumab emtansine (T-DM1): mechanism of action of its cytotoxic component retained with improved tolerability. Toxicol Appl Pharmacol. 2013 Dec 1;273(2):298-313. doi: 10.1016/j.taap.2013.09.003. Epub 2013 Sep 12.
8 Cerner Multum, Inc. "Australian Product Information.".
9 European Medicines Agency "Summary on compassionate use. Remdesivir Gilead.".
10 Product Information. Hivid (zalcitabine). Roche Laboratories, Nutley, NJ.
11 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
12 Bannister SJ, Houser VP, Hulse JD, Kisicki JC, Rasmussen JG "Evaluation of the potential for interactions of paroxetine with diazepam, cimetidine, warfarin, and digoxin." Acta Psychiatr Scand Suppl 350 (1989): 102-6. [PMID: 2530759]
13 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
14 Product Information. Xcopri (cenobamate). SK Life Science, Inc., Paramus, NJ.
15 Product Information. Accolate (zafirlukast). Zeneca Pharmaceuticals, Wilmington, DE.
16 Canadian Pharmacists Association.
17 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
18 Bodmer M, Sulz M, Stadlmann S, Droll A, Terracciano L, Krahenbuhl S "Fatal liver failure in an adult patient with acute lymphoblastic leukemia following treatment with L-asparaginase." Digestion 74 (2006): epub. [PMID: 16988508]
19 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
20 Product Information. Brukinsa (zanubrutinib). BeiGene USA, Inc, San Mateo, CA.
21 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
22 Product Information. Acular (ketorolac). Allergan Inc, Irvine, CA.
23 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
24 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]