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Identification
NameTrastuzumab emtansine
Accession NumberDB05773
TypeBiotech
GroupsApproved
DescriptionTrastuzumab emtansine, formerly called Trastuzumab-DM1 (T-DM1) is a first-in-class HER2 antibody drug conjugate (ADC) comprised of Genentech's trastuzumab antibody linked to ImmunoGen's cell-killing agent, DM1. T-DM1 combines two strategies-- anti-HER2 activity and targeted intracellular delivery of the potent anti-microtubule agent, DM1 (a maytansine derivative)--to produce cell cycle arrest and apoptosis. Trastuzumab emtansine is marketed under the brand name Kadcyla and is indicated for use in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment. The FDA label has two precautions. First that trastuzumab emtansine and trastuzumab cannot be interchanged. Second that there is a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity.
Protein structureNo structure small
Related Articles
Protein chemical formulaNot Available
Protein average weightNot Available
SequencesNot Available
Synonyms
Ado-trastuzumab
Ado-trastuzumab emtansine
T-DM1
Trastuzumab emtansine
Trastuzumab-DM1
Trastuzumab-MCC-DM1
External Identifiers
  • PRO-132365
  • PRO132365
  • RG-3502
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Kadcylainjection, powder, lyophilized, for solution20 mg/mLintravenousGenentech, Inc.2013-02-22Not applicableUs
Kadcylainjection, powder, lyophilized, for solution20 mg/mLintravenousGenentech, Inc.2013-02-22Not applicableUs
Kadcylapowder for solution20 mgintravenousHoffmann La Roche Limited2013-10-09Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIISE2KH7T06F
CAS number1018448-65-1
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationUsed in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment.
PharmacodynamicsTrastuzumab emtansine was evaluated in two Herceptin-responsive and one Herceptin-resistant breast tumor models. In the Herceptin-responsive models, Trastuzumab-DM1 caused complete tumor regression in all mice, whereas Herceptin alone slowed tumor growth. In the Herceptin- resistant model, Herceptin alone had no effect on tumor growth. In contrast, Trastuzumab-DM1 caused >90% tumor reduction in all mice. In this Herceptin- resistant model, tumor regrowth was observed after cessation of Trastuzumab- DM1 treatment, yet regression re-occurred when dosing was resumed. The effect was specific for HER2-positive tumors. Thus the physiological effects of trastuzumab emtansine are cell cycle arrest and cell death by apoptosis.
Mechanism of actionTrastuzumab emtansine is a HER2 antibody drug conjugate. The antibody portion is trastuzumab, which is humanized anti-HER2 IgG1, and produced in the mammalian Chinese Hamster Ovary cells. The drug portion is DM1, which is a maytansine derivative that inhibits microtubules. These two portions are covalently connected by 4-[N-maleimidomethyl] cyclohexane-1-carboxylate (MCC), which is a stable thioether linker. Together MCC and DM1 are called emtansine and are produced by chemical synthesis. Trastuzumab emtansine binds to the HER2 receptor’s sub-domain IV and goes into the cell by receptor-mediated endocytosis. Lysosomes degrade trastuzumab emtansine and release DM1. DM1 binds to tubulin in microtubules and inhibits microtubule function producing cell arrest and apoptosis. As well, similar to trastuzumab, in vitro studies have shown that both HER2 receptor signalling inhibition and antibody-dependent cytotoxicity are mediated by trastuzumab emtansine.
Related Articles
AbsorptionThe absorption/ bioavailability should be close to 100% since trastuzumab emtansine is administered IV.
Volume of distribution

The volume of distribution of trastuzumab emtansine is about 3.13 L.

Protein bindingDM1 has a plasma protein binding value of 93%.
Metabolism

Trastuzumab emtansine undergoes lysosomal degradation to MCC-DM1, Lys-MCC-DM1, and DM1. All of these products are detected at low levels in the plasma. DM1 undergoes further degradation by CYP3A4 and CYP3A5, but DM1 does not induce or inhibit any of the CYP450 enzymes.

Route of eliminationThe route of elimination has not yet been fully elucidated.
Half lifeTrastuzumab emtansine has a long half life of about 4 days.
Clearance

After IV infusion, trastuzumab emtansine has a clearance of 0.68 L/day.

ToxicityThe FDA label includes a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionintravenous20 mg/mL
Powder for solutionintravenous20 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General References
  1. Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, Blattler WA, Lambert JM, Chari RV, Lutz RJ, Wong WL, Jacobson FS, Koeppen H, Schwall RH, Kenkare-Mitra SR, Spencer SD, Sliwkowski MX: Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer Res. 2008 Nov 15;68(22):9280-90. doi: 10.1158/0008-5472.CAN-08-1776. [PubMed:19010901 ]
External Links
ATC CodesL01XC14
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (428 KB)
MSDSDownload (381 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.
AfatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Alfentanil.
AmantadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amantadine.
Aminohippuric acidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Amiodarone.
AmitriptylineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amsacrine.
AprepitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Aprepitant.
AstemizoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Atazanavir.
AtenololThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Trastuzumab emtansine can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Azithromycin.
BelimumabThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Belimumab.
BenzocaineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Bepridil.
BevacizumabBevacizumab may increase the cardiotoxic activities of Trastuzumab emtansine.
BexaroteneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Biperiden.
BoceprevirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Boceprevir.
BortezomibThe metabolism of Trastuzumab emtansine can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Caspofungin.
CeritinibThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ceritinib.
ChloroquineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Clarithromycin.
ClemastineThe metabolism of Trastuzumab emtansine can be decreased when combined with Clemastine.
ClofazimineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Clomipramine.
ClotrimazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Clozapine.
CobicistatThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Cobicistat.
ColchicineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Trastuzumab emtansine.
CyclosporineThe metabolism of Trastuzumab emtansine can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dactinomycin.
DarunavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Darunavir.
DasatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Daunorubicin.
DeferasiroxThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Trastuzumab emtansine can be decreased when combined with Delavirdine.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Trastuzumab emtansine.
DesipramineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Trastuzumab emtansine.
DesloratadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Diclofenac.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.
DigoxinDigoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.
DihydroergotamineThe metabolism of Trastuzumab emtansine can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Trastuzumab emtansine can be decreased when combined with Diltiazem.
DipyridamoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dipyridamole.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Trastuzumab emtansine.
DoxazosinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Doxorubicin.
DoxycyclineThe metabolism of Trastuzumab emtansine can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dronabinol.
DronedaroneThe metabolism of Trastuzumab emtansine can be decreased when combined with Dronedarone.
EfavirenzThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Elbasvir.
EnalaprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Enzalutamide.
ErgonovineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ergotamine.
ErythromycinThe metabolism of Trastuzumab emtansine can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Eslicarbazepine acetate.
EstramustineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Estrone.
EtoposideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Etravirine.
FelodipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fidaxomicin.
FingolimodTrastuzumab emtansine may increase the immunosuppressive activities of Fingolimod.
FluconazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Fluconazole.
FluoxetineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Flurazepam.
FluvoxamineThe metabolism of Trastuzumab emtansine can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Trastuzumab emtansine can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Trastuzumab emtansine can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Gefitinib.
GenisteinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Hydrocortisone.
IdelalisibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Imipramine.
IndinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Indinavir.
IndomethacinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Indomethacin.
IsavuconazoniumThe metabolism of Trastuzumab emtansine can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Trastuzumab emtansine can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Itraconazole.
IvacaftorThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ketoconazole.
LansoprazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lapatinib.
LeflunomideThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Leflunomide.
LevofloxacinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Levofloxacin.
LevothyroxineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Lopinavir.
LoratadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Losartan.
LovastatinThe metabolism of Trastuzumab emtansine can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Lumacaftor.
MaprotilineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Meprobamate.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Trastuzumab emtansine.
MethadoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Methadone.
MetoprololThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Metoprolol.
MibefradilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Midazolam.
MifepristoneThe metabolism of Trastuzumab emtansine can be decreased when combined with Mifepristone.
MitomycinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Mitoxantrone.
ModafinilThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Morphine.
NafcillinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Nafcillin.
NaltrexoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Naringenin.
NatalizumabThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Natalizumab.
NefazodoneThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Nefazodone.
NelfinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Nelfinavir.
NeostigmineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Trastuzumab emtansine can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Nifedipine.
NilotinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Nilotinib.
NisoldipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Norethisterone.
OlaparibThe metabolism of Trastuzumab emtansine can be decreased when combined with Olaparib.
OmeprazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Trastuzumab emtansine.
P-NitrophenolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Palbociclib.
Palmitic AcidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Paroxetine.
PentobarbitalThe metabolism of Trastuzumab emtansine can be increased when combined with Pentobarbital.
PerindoprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Phenobarbital.
PhenytoinThe metabolism of Trastuzumab emtansine can be increased when combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Trastuzumab emtansine.
PimozideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Pimozide.
Platelet Activating FactorThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Platelet Activating Factor.
PonatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Posaconazole.
PravastatinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Prednisone.
PrimidoneThe metabolism of Trastuzumab emtansine can be increased when combined with Primidone.
ProbenecidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Progesterone.
PromethazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Protriptyline.
QuercetinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quercetin.
QuinacrineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quinine.
Rabies vaccineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Rabies vaccine.
RanitidineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Reserpine.
RifabutinThe metabolism of Trastuzumab emtansine can be increased when combined with Rifabutin.
RifampicinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Rifampicin.
RifapentineThe metabolism of Trastuzumab emtansine can be increased when combined with Rifapentine.
RilpivirineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Rilpivirine.
RitonavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ritonavir.
RoflumilastRoflumilast may increase the immunosuppressive activities of Trastuzumab emtansine.
RolapitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Rolapitant.
SaquinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Saquinavir.
ScopolamineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sertraline.
SildenafilThe metabolism of Trastuzumab emtansine can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Simvastatin.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Trastuzumab emtansine.
SirolimusThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Sirolimus.
SorafenibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sorafenib.
SpironolactoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Streptozocin.
SulfinpyrazoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Sulfisoxazole.
SumatriptanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Tacrine.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trastuzumab emtansine.
TamoxifenThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Taurocholic Acid.
TelaprevirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Telaprevir.
TelithromycinThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Telithromycin.
TelmisartanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Temsirolimus.
TerazosinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Terfenadine.
TesmilifeneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Testosterone.
TicagrelorThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Trastuzumab emtansine can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tocilizumab.
TofacitinibTrastuzumab emtansine may increase the immunosuppressive activities of Tofacitinib.
TolvaptanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Tolvaptan.
TrastuzumabTrastuzumab may increase the neutropenic activities of Trastuzumab emtansine.
TrazodoneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Troleandomycin.
VenlafaxineThe metabolism of Trastuzumab emtansine can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Trastuzumab emtansine can be decreased when combined with Verapamil.
VinblastineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Vinorelbine.
VoriconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Voriconazole.
ZimelidineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Zimelidine.
ZiprasidoneThe metabolism of Trastuzumab emtansine can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antibody
General Function:
Transmembrane signaling receptor activity
Specific Function:
Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-...
Gene Name:
ERBB2
Uniprot ID:
P04626
Molecular Weight:
137909.27 Da
References
  1. Barginear MF, John V, Budman DR: Trastuzumab-DM1: a clinical update of the novel antibody-drug conjugate for HER2-overexpressing breast cancer. Mol Med. 2013 Jan 22;18:1473-9. doi: 10.2119/molmed.2012.00302. [PubMed:23196784 ]
  2. Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, Blattler WA, Lambert JM, Chari RV, Lutz RJ, Wong WL, Jacobson FS, Koeppen H, Schwall RH, Kenkare-Mitra SR, Spencer SD, Sliwkowski MX: Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer Res. 2008 Nov 15;68(22):9280-90. doi: 10.1158/0008-5472.CAN-08-1776. [PubMed:19010901 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
Comments
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Drug created on November 18, 2007 11:27 / Updated on August 17, 2016 12:24