Identification

Name
Trastuzumab emtansine
Accession Number
DB05773
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Description

Trastuzumab 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 chemical formula
Not Available
Protein average weight
Not Available
Sequences
Not Available
Synonyms
  • Ado-trastuzumab
  • Ado-trastuzumab emtansine
  • T-DM1
  • Trastuzumab emtansine
  • Trastuzumab-DM1
  • Trastuzumab-MCC-DM1
External IDs
PRO-132365 / PRO132365 / RG-3502
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
KadcylaInjection, powder, lyophilized, for solution20 mg/mLIntravenousGenentech, Inc.2013-02-22Not applicableUs
KadcylaPowder, for solution100 mgIntravenousHoffmann La Roche2013-10-09Not applicableCanada
KadcylaInjection, powder, lyophilized, for solution20 mg/mLIntravenousGenentech, Inc.2013-02-22Not applicableUs
KadcylaPowder, for solution160 mgIntravenousHoffmann La RocheNot applicableNot applicableCanada
Categories
UNII
SE2KH7T06F
CAS number
1018448-65-1

Pharmacology

Indication

Used 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.

Associated Conditions
Pharmacodynamics

Trastuzumab 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 action

Trastuzumab 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.

TargetActionsOrganism
AReceptor tyrosine-protein kinase erbB-2
antibody
Human
Absorption

The 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 binding

DM1 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 elimination

The route of elimination has not yet been fully elucidated.

Half life

Trastuzumab emtansine has a long half life of about 4 days.

Clearance

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

Toxicity

The 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Trastuzumab emtansine.Approved
AcetaminophenThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Acetaminophen.Approved
Acetyl sulfisoxazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Trastuzumab emtansine.Approved
AldesleukinThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Aldesleukin.Approved
AmiodaroneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amiodarone.Approved, Investigational
AmlodipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amlodipine.Approved
AnakinraThe risk or severity of adverse effects can be increased when Anakinra is combined with Trastuzumab emtansine.Approved
AncestimThe risk or severity of cytotoxicity can be increased when Ancestim is combined with Trastuzumab emtansine.Approved, Investigational, Withdrawn
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Anthrax immune globulin human.Approved
ApalutamideThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Apalutamide.Approved, Investigational
AprepitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Trastuzumab emtansine can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of rhabdomyolysis can be increased when Trastuzumab emtansine is combined with Atorvastatin.Approved
Bacillus calmette-guerin substrain connaught live antigenThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Bacillus calmette-guerin substrain connaught live antigen.Approved, Investigational
Bacillus calmette-guerin substrain tice live antigenThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Bacillus calmette-guerin substrain tice live antigen.Approved
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Trastuzumab emtansine.Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Beclomethasone dipropionate.Approved, Investigational
BelimumabThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Belimumab.Approved
Benzyl alcoholThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Benzyl alcohol.Approved
BepridilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabBevacizumab may increase the cardiotoxic activities of Trastuzumab emtansine.Approved, Investigational
BoceprevirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Trastuzumab emtansine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Bosentan.Approved, Investigational
BudesonideThe risk or severity of adverse effects can be increased when Budesonide is combined with Trastuzumab emtansine.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Trastuzumab emtansine.Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Trastuzumab emtansine.Approved
CarbamazepineThe metabolism of Carbamazepine can be decreased when combined with Trastuzumab emtansine.Approved, Investigational
CarvedilolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Carvedilol.Approved, Investigational
CeritinibThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ceritinib.Approved
CerivastatinThe risk or severity of rhabdomyolysis can be increased when Trastuzumab emtansine is combined with Cerivastatin.Approved, Withdrawn
CetuximabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Trastuzumab emtansine.Approved
ClarithromycinThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Clarithromycin.Approved
Clostridium tetani toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated).Approved
ClotrimazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Clozapine.Approved
CobicistatThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Cobicistat.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Trastuzumab emtansine.Approved, Investigational
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated).Approved
CrizotinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Crizotinib.Approved
CurcuminThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Curcumin.Approved, Investigational
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Trastuzumab emtansine.Approved, Investigational
CyclosporineThe metabolism of Cyclosporine can be decreased when combined with Trastuzumab emtansine.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
DabrafenibThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Dabrafenib.Approved, Investigational
DarunavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Darunavir.Approved
DasatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Trastuzumab emtansine can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Trastuzumab emtansine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Dexamethasone is combined with Trastuzumab emtansine.Approved, Investigational, Vet Approved
DexniguldipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dexniguldipine.Experimental
DexverapamilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dexverapamil.Experimental
DigitoxinDigitoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
DihydroergotamineThe metabolism of Trastuzumab emtansine can be decreased when combined with Dihydroergotamine.Approved, Investigational
DiltiazemThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Diltiazem.Approved, Investigational
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Trastuzumab emtansine.Approved, Investigational
DoxazosinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Doxazosin.Approved
DoxycyclineThe metabolism of Trastuzumab emtansine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Trastuzumab emtansine can be decreased when combined with Dronedarone.Approved
EmopamilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Emopamil.Experimental
EnzalutamideThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Trastuzumab emtansine can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Trastuzumab emtansine.Approved, Investigational
EverolimusThe risk or severity of adverse effects can be increased when Everolimus is combined with Trastuzumab emtansine.Approved
FelodipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FingolimodTrastuzumab emtansine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Fluconazole.Approved, Investigational
FluoxetineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fluoxetine.Approved, Vet Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Fluticasone propionate.Approved
FluvoxamineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Trastuzumab emtansine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Trastuzumab emtansine can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fusidic Acid.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with G17DT.Investigational
GallopamilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Gallopamil.Investigational
GanciclovirThe metabolism of Ganciclovir can be decreased when combined with Trastuzumab emtansine.Approved, Investigational
GemcitabineThe risk or severity of adverse effects can be increased when Gemcitabine is combined with Trastuzumab emtansine.Approved
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Trastuzumab emtansine.Approved, Investigational
GI-5005The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with GI-5005.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
GlyburideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Glyburide.Approved
GlycerinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Glycerin.Approved, Investigational
Gramicidin DThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Gramicidin D.Approved
Hepatitis A VaccineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Hepatitis A Vaccine.Approved
Hepatitis B Vaccine (Recombinant)The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Hepatitis B Vaccine (Recombinant).Approved, Withdrawn
Human rabies virus immune globulinThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Human rabies virus immune globulin.Approved
HydrocodoneThe metabolism of Hydrocodone can be decreased when combined with Trastuzumab emtansine.Approved, Illicit
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Trastuzumab emtansine.Approved, Vet Approved
Hydrocortisone acetateThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Hydrocortisone acetate.Approved, Vet Approved
Hydrocortisone butyrateThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Hydrocortisone butyrate.Approved, Vet Approved
IbuprofenThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ibuprofen.Approved
IdelalisibThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Idelalisib.Approved
ImatinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Imatinib.Approved
Immune Globulin HumanThe risk or severity of adverse effects can be increased when Immune Globulin Human is combined with Trastuzumab emtansine.Approved, Investigational
IndinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Indinavir.Approved
INGN 201The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with INGN 225.Investigational
Interferon alfa-n3The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Interferon alfa-n3.Approved, Investigational
IrinotecanThe risk or severity of adverse effects can be increased when Irinotecan is combined with Trastuzumab emtansine.Approved, Investigational
IsavuconazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Trastuzumab emtansine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Isradipine.Approved, Investigational
ItraconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ivacaftor.Approved
Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated).Approved
KetoconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ketoconazole.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
LeflunomideThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Leflunomide.Approved, Investigational
LidocaineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lidocaine.Approved, Vet Approved
LipegfilgrastimTrastuzumab emtansine may increase the myelosuppressive activities of Lipegfilgrastim.Approved, Investigational
LomerizineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lomerizine.Experimental
LoperamideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Lopinavir.Approved
LoratadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Loratadine.Approved, Investigational
LorpiprazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lorpiprazole.Approved
LosartanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Losartan.Approved
LovastatinThe risk or severity of rhabdomyolysis can be increased when Trastuzumab emtansine is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Lumacaftor.Approved
MetamizoleThe risk or severity of myelosuppression can be increased when Metamizole is combined with Trastuzumab emtansine.Approved, Investigational, Withdrawn
MethimazoleThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Methimazole.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Trastuzumab emtansine.Approved, Vet Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
MevastatinThe risk or severity of rhabdomyolysis can be increased when Trastuzumab emtansine is combined with Mevastatin.Experimental
MibefradilThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MifepristoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Mitotane.Approved
NatalizumabThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Natalizumab.Approved, Investigational
NefazodoneThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Nelfinavir.Approved
NetupitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Trastuzumab emtansine can be increased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nicardipine.Approved, Investigational
NiguldipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Niguldipine.Experimental
NilotinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Nilotinib.Approved, Investigational
NimodipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nimodipine.Approved, Investigational
NisoldipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nisoldipine.Approved
NitrendipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nitrendipine.Approved, Investigational
OcrelizumabOcrelizumab may increase the immunosuppressive activities of Trastuzumab emtansine.Approved, Investigational
OlaparibThe metabolism of Trastuzumab emtansine can be decreased when combined with Olaparib.Approved
OleandrinOleandrin may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental, Investigational
OmalizumabThe risk or severity of adverse effects can be increased when Omalizumab is combined with Trastuzumab emtansine.Approved, Investigational
OmeprazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Trastuzumab emtansine.Approved, Vet Approved
PalbociclibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Palbociclib.Approved, Investigational
PaliferminThe therapeutic efficacy of Palifermin can be decreased when used in combination with Trastuzumab emtansine.Approved
ParoxetineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Paroxetine.Approved, Investigational
PegaspargaseThe risk or severity of adverse effects can be increased when Pegaspargase is combined with Trastuzumab emtansine.Approved, Investigational
Peginterferon alfa-2aThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Peginterferon alfa-2a.Approved, Investigational
Peginterferon alfa-2bThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Trastuzumab emtansine can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
PhenobarbitalThe metabolism of Trastuzumab emtansine can be increased when combined with Phenobarbital.Approved, Investigational
PhenytoinThe metabolism of Trastuzumab emtansine can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Trastuzumab emtansine.Approved, Investigational
PitavastatinThe risk or severity of rhabdomyolysis can be increased when Trastuzumab emtansine is combined with Pitavastatin.Approved
PosaconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe risk or severity of rhabdomyolysis can be increased when Trastuzumab emtansine is combined with Pravastatin.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Trastuzumab emtansine.Approved, Vet Approved
PrimidoneThe metabolism of Trastuzumab emtansine can be increased when combined with Primidone.Approved, Vet Approved
PromethazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Promethazine.Approved, Investigational
PropafenoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Propafenone.Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
Rabies virus inactivated antigen, AThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Rabies virus inactivated antigen, A.Approved, Investigational
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Trastuzumab emtansine.Approved, Investigational
RanitidineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Trastuzumab emtansine can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Trastuzumab emtansine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Trastuzumab emtansine can be increased when combined with Rifapentine.Approved, Investigational
RindopepimutThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Rindopepimut.Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Trastuzumab emtansine.Approved
Rotavirus VaccineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Rotavirus Vaccine.Approved
Rubella virus vaccineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Rubella virus vaccine.Approved, Investigational
RucaparibThe metabolism of Trastuzumab emtansine can be decreased when combined with Rucaparib.Approved, Investigational
Salmonella typhi ty2 vi polysaccharide antigenThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Salmonella typhi ty2 vi polysaccharide antigen.Approved
Salmonella typhi Ty21a live antigenThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Salmonella typhi ty21a live antigen.Approved
SaquinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Trastuzumab emtansine can be decreased when used in combination with Sarilumab.Approved, Investigational
SildenafilThe metabolism of Trastuzumab emtansine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe risk or severity of rhabdomyolysis can be increased when Trastuzumab emtansine is combined with Simvastatin.Approved
SRP 299The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Stiripentol.Approved
SulfasalazineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Sulfasalazine.Approved
SulfisoxazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusTacrolimus may increase the immunosuppressive activities of Trastuzumab emtansine.Approved, Investigational
TecemotideThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Tecemotide.Investigational
TelaprevirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Telithromycin.Approved
TetrandrineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Tetrandrine.Experimental
TG4010The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with TG4010.Investigational
TiclopidineThe metabolism of Trastuzumab emtansine can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tocilizumab.Approved
TofacitinibTrastuzumab emtansine may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Trastuzumab emtansine.Approved, Investigational
Typhoid VaccineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Typhoid Vaccine.Approved
ValaciclovirThe metabolism of Valaciclovir can be decreased when combined with Trastuzumab emtansine.Approved, Investigational
Varicella Zoster Vaccine (Live/Attenuated)The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Varicella Zoster Vaccine (Live/Attenuated).Approved
VemurafenibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Verapamil.Approved
VoriconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Voriconazole.Approved, Investigational
Yellow Fever VaccineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Yellow Fever Vaccine.Approved, Investigational
ZidovudineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Zidovudine.Approved
ZiprasidoneThe metabolism of Trastuzumab emtansine can be decreased when combined with Ziprasidone.Approved
Food Interactions
Not Available

References

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
KEGG Drug
D09980
PubChem Substance
347910224
ChEMBL
CHEMBL1743082
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Trastuzumab_emtansine
ATC Codes
L01XC14 — Trastuzumab emtansine
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (428 KB)
MSDS
Download (381 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentHER2 Positive Breast Cancers1
1Active Not RecruitingTreatmentHER2 Positive Breast Cancers / Her2-negative Metastatic Breast Cancer / HER2-positive Metastatic Breast Cancer / Locally Advanced or Early Breast Cancer1
1Active Not RecruitingTreatmentHER2/Neu Positive / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1Active Not RecruitingTreatmentHer2-Positive Breast Cancer / Recurrent Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1Active Not RecruitingTreatmentNeoplasms, Breast1
1CompletedTreatmentCancer, Breast2
1CompletedTreatmentMetastatic Breast Cancer (MBC)2
1RecruitingTreatmentAdvanced Breast Cancer1
1RecruitingTreatmentCancer, Breast3
1RecruitingTreatmentHER2 Positive Breast Carcinoma / Recurrent Breast Carcinoma / Stage III Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1RecruitingTreatmentMetastatic Breast Cancer (MBC) / Recurrent Breast Cancer1
1, 2Active Not RecruitingTreatmentCancer, Advanced / Cancer, Breast / Colorectal Cancers / Esophageal Cancers / Malignant Neoplasm of Stomach1
1, 2Active Not RecruitingTreatmentCancer, Breast / Metastatic Breast Cancer (MBC)1
1, 2CompletedTreatmentMetastatic Breast Cancer (MBC)2
1, 2RecruitingTreatmentBrain Cancer / Brain Metastasis / Cancer, Breast1
1, 2RecruitingTreatmentCancer, Breast2
2Active Not RecruitingDiagnosticHER-2 Positive Breast Cancer1
2Active Not RecruitingTreatmentCancer, Breast3
2Active Not RecruitingTreatmentEstrogen Receptor Negative / Estrogen Receptor Status / HER2 Positive Breast Carcinoma / Progesterone Receptor Negative / Progesterone Receptor Status / Stage I Breast Cancer AJCC v7 / Stage I Breast Carcinoma / Stage IA Breast Cancer / Stage IA Breast Cancer AJCC v7 / Stage IB Breast Cancer / Stage IB Breast Cancer AJCC v7 / Stage II Breast Cancer / Stage II Breast Cancer AJCC v6 and v7 / Stage IIA Breast Cancer / Stage IIA Breast Cancer AJCC v6 and v7 / Stage IIB Breast Cancer / Stage IIB Breast Cancer AJCC v6 and v7 / Stage III Breast Cancer / Stage III Breast Cancer AJCC V7 / Stage IIIA Breast Cancer / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v71
2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)2
2CompletedTreatmentBladder Cancer, Pancreas Cancer, Cholangiocellular Carcinoma / Bladder Cancers / Cholangiocellular Carcinoma / Malignant Neoplasm of Pancreas1
2CompletedTreatmentBreast Cancer, Gastric Cancer / Tumors, Solid1
2CompletedTreatmentCancer, Breast2
2CompletedTreatmentMetastatic Breast Cancer (MBC)3
2Not Yet RecruitingTreatmentBreast Cancer Stage / Cancer, Breast / HER2 Positive Breast Carcinoma / Her2-Positive Breast Cancer / Metastatic Breast Cancer (MBC) / Recurrent Breast Cancer1
2Not Yet RecruitingTreatmentCancer, Breast1
2Not Yet RecruitingTreatmentMetastatic HER2-positive Breast Cancer With Brain Metastasis1
2RecruitingTreatmentAdvanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Bladder Carcinoma / Carcinoma, Breast / Carcinoma, Colorectal / Carcinoma, Pancreatic / Cervical Carcinoma / Colon Carcinoma / Endometrial Carcinoma / Gastric Carcinoma / Gliomas / Head and Neck Carcinoma / Liver and Intrahepatic Bile Duct Carcinoma / Lung, Carcinoma / Malignant Lymphomas / Malignant Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Prostate Cancer / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Plasma Cell Myeloma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Solid Neoplasm / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Carcinoma / Refractory Lymphomas / Refractory Malignant Neoplasm / Refractory Malignant Solid Neoplasm / Refractory Plasma Cell Myeloma / Renal Carcinoma / Skin Carcinoma / Solid Neoplasms / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2RecruitingTreatmentBladder Cancers / Lung Cancers / Solid Tumor Cancers / Urinary Tract Cancers1
2RecruitingTreatmentCancer, Breast / HER-2 Positive Breast Cancer / Stage II Breast Cancer / Stage III Breast Cancer1
2RecruitingTreatmentCancer, Breast / Neoplasms Metastasis1
2RecruitingTreatmentCancer, Breast / Neoplasms, Breast / Tumors, Breast1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2RecruitingTreatmentMetastatic Colorectal Cancers1
2WithdrawnTreatmentCancer, Breast1
2, 3CompletedTreatmentMalignant Neoplasm of Stomach1
2, 3RecruitingTreatmentEarly-Stage Breast Carcinoma / HER-2 Positive Breast Cancer1
3Active Not RecruitingTreatmentCancer, Breast3
3Active Not RecruitingTreatmentCancer, Breast / Neoplasms, Breast1
3CompletedTreatmentCancer, Breast3
3CompletedTreatmentMetastatic Breast Cancer (MBC)1
3RecruitingTreatmentCancer, Breast2
4RecruitingBasic ScienceHER2 Positive Breast Cancer, Metastatic Breast Cancer, Locally Advanced Breast Cancer1
Not AvailableActive Not RecruitingDiagnosticBone Metastases / Hepatic Metastases / Her2-Positive Breast Cancer / Lung Cancer Metastatic / Recurrent Breast Cancer / Soft Tissue Metastases / Stage IV Breast Cancer1
Not AvailableNo Longer AvailableNot AvailableMetastatic Breast Cancer (MBC)1
Not AvailableRecruitingNot AvailableCancer, Breast / Pregnancy1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous20 mg/mL
Powder, for solutionIntravenous100 mg
Powder, for solutionIntravenous160 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not 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, alt...
Gene Name
ERBB2
Uniprot ID
P04626
Uniprot Name
Receptor tyrosine-protein kinase erbB-2
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
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Kuper JI, D'Aprile M: Drug-Drug interactions of clinical significance in the treatment of patients with Mycobacterium avium complex disease. Clin Pharmacokinet. 2000 Sep;39(3):203-14. [PubMed:11020135]
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
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
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da

Drug created on November 18, 2007 11:27 / Updated on August 15, 2018 09:53