Identification

Name
Trastuzumab emtansine
Accession Number
DB05773
Type
Biotech
Groups
Approved
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
KadcylaPowder, for solution20 mgIntravenousHoffmann La Roche2013-10-09Not applicableCanada
KadcylaInjection, powder, lyophilized, for solution20 mg/mLIntravenousGenentech, Inc.2013-02-22Not applicableUs
KadcylaInjection, powder, lyophilized, for solution20 mg/mLIntravenousGenentech, Inc.2013-02-22Not applicableUs
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.

Structured Indications
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
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
AmiodaroneThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Amiodarone.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
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Trastuzumab emtansine.Investigational
BelimumabThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Belimumab.Approved
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
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Trastuzumab emtansine.Approved
CarbamazepineThe metabolism of Trastuzumab emtansine can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ceritinib.Approved
ClarithromycinThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Clarithromycin.Approved
ClemastineThe metabolism of Trastuzumab emtansine can be decreased when combined with Clemastine.Approved
Clostridium tetani toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Trastuzumab emtansine.Approved
ClotrimazoleThe metabolism of Trastuzumab emtansine can be decreased when combined 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 Trastuzumab emtansine can be increased when it is combined with Conivaptan.Approved, Investigational
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Trastuzumab emtansine.Approved
CrizotinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Trastuzumab emtansine.Approved, Investigational
CyclosporineThe metabolism of Trastuzumab emtansine can be decreased when combined with Cyclosporine.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
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
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
DiltiazemThe metabolism of Trastuzumab emtansine can be decreased when combined with Diltiazem.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Trastuzumab emtansine.Approved, Investigational
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
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, 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
FluvoxamineThe metabolism of Trastuzumab emtansine can be decreased when 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
Fusidic AcidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fusidic Acid.Approved
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Trastuzumab emtansine.Investigational
GI-5005The therapeutic efficacy of GI-5005 can be decreased when used in combination with Trastuzumab emtansine.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
Hepatitis A VaccineThe therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Trastuzumab emtansine.Approved
Hepatitis B Vaccine (Recombinant)The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Trastuzumab emtansine.Approved, Withdrawn
IdelalisibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Imatinib.Approved
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 therapeutic efficacy of INGN 201 can be decreased when used in combination with Trastuzumab emtansine.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Trastuzumab emtansine.Investigational
IsavuconazoniumThe metabolism of Trastuzumab emtansine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Trastuzumab emtansine can be decreased when combined with Isradipine.Approved
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
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
LopinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Lopinavir.Approved
LovastatinThe metabolism of Trastuzumab emtansine can be decreased when 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 adverse effects can be increased when Metamizole is combined with Trastuzumab emtansine.Investigational, Withdrawn
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
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
NevirapineThe metabolism of Trastuzumab emtansine can be increased when combined with Nevirapine.Approved
NilotinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Nilotinib.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
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
PentobarbitalThe metabolism of Trastuzumab emtansine can be increased when combined with Pentobarbital.Approved, 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
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
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
PrimidoneThe metabolism of Trastuzumab emtansine can be increased when combined with Primidone.Approved, Vet Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Trastuzumab emtansine.Experimental
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Trastuzumab emtansine.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
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
RindopepimutThe therapeutic efficacy of Rindopepimut can be decreased when used in combination with Trastuzumab emtansine.Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Trastuzumab emtansine.Approved
Rotavirus VaccineThe therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Trastuzumab emtansine.Approved
Rubella virus vaccineThe therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Trastuzumab emtansine.Approved
Salmonella typhi ty21a live antigenThe therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Trastuzumab emtansine.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
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
SimeprevirThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Simeprevir.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Trastuzumab emtansine.Approved
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Trastuzumab emtansine.Investigational
St. John's WortThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trastuzumab emtansine.Approved, Investigational
TecemotideThe therapeutic efficacy of Tecemotide can be decreased when used in combination with Trastuzumab emtansine.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
TG4010The therapeutic efficacy of TG4010 can be decreased when used in combination with Trastuzumab emtansine.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
VenlafaxineThe metabolism of Trastuzumab emtansine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Trastuzumab emtansine can be decreased when 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 therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Trastuzumab emtansine.Approved
ZiprasidoneThe metabolism of Trastuzumab emtansine can be decreased when combined with Ziprasidone.Approved
Zoster vaccineThe therapeutic efficacy of Zoster vaccine can be decreased when used in combination with Trastuzumab emtansine.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/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
1CompletedTreatmentCancer, Breast2
1CompletedTreatmentMetastatic Breast Cancer (MBC)2
1RecruitingTreatmentAdvanced Breast Cancer1
1RecruitingTreatmentCancer, Breast2
1RecruitingTreatmentHER2 Positive Breast Cancers / Her2-negative Metastatic Breast Cancer / HER2-positive Metastatic Breast Cancer / Locally Advanced or Early Breast Cancer1
1RecruitingTreatmentMetastatic Breast Cancer (MBC) / Recurrent Breast Cancer1
1RecruitingTreatmentNeoplasms, Breast1
1, 2CompletedTreatmentMetastatic Breast Cancer (MBC)2
1, 2RecruitingTreatmentBrain Cancer / Brain Metastasis / Cancer, Breast1
1, 2RecruitingTreatmentCancer, Advanced / Cancer, Breast / Colorectal Cancers / Esophageal Cancers / Malignant Neoplasm of Stomach1
1, 2RecruitingTreatmentCancer, Breast2
1, 2RecruitingTreatmentCancer, Breast / Metastatic Breast Cancer (MBC)1
1, 2RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentCancer, Breast2
2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)2
2CompletedTreatmentBreast Cancer, Gastric Cancer / Tumors, Solid1
2CompletedTreatmentCancer, Breast2
2CompletedTreatmentMetastatic Breast Cancer (MBC)3
2Not Yet RecruitingTreatmentMetastatic HER2-positive Breast Cancer With Brain Metastasis1
2RecruitingDiagnosticHER-2 Positive Breast Cancer1
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 Cancer, Pancreas Cancer, Cholangiocellular Carcinoma1
2RecruitingTreatmentBladder Cancers / Lung Cancers / Solid Tumor Cancers / Urinary Tract Cancers1
2RecruitingTreatmentCancer, Breast1
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
2RecruitingTreatmentEstrogen Receptor Negative / HER2 Positive Breast Carcinoma / Progesterone Receptor Negative / Stage IB Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer / Stage IIIC Breast Cancer1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
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, Breast1
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 solutionIntravenous20 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
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
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 November 19, 2017 20:33