Trastuzumab Emtansine

Summary

Trastuzumab Emtansine (CHEMBL1743082) is an approved antibody drug conjugate (ATC L01FD03); indicated across 14 conditions including breast carcinoma and neoplasm; with CIViC clinical evidence for 16 variant-indication associations (e.g. ERBB2 Amplification in her2-receptor positive breast cancer).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Antibody drug conjugate
• ATC class: L01FD03
• Indications: 14 conditions
• Clinical trials: 115
• Precision-oncology evidence (CIViC): 16 variant–indication associations

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1743082
Name	Trastuzumab Emtansine
Type	Antibody drug conjugate
Max phase	4
ATC	L01FD03

Also known as: Ado-trastuzumab emtansine, Kadcyla, PRO-132365, RG-3502, T-dm1, TDM-1, TDM1, Trastuzumab emtansina, Trastuzumab emtansine, TRASTUZUMAB-MCC-DM1 T-DM1, TRASTUZUMAB EMTANSINE

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

14 indications (6 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
breast carcinoma	4	MONDO:0004989	EFO:0000305
neoplasm	4	MONDO:0005070	EFO:0000616
breast neoplasm	4	MONDO:0021100	EFO:0003869
HER2 positive breast carcinoma	4	MONDO:0006244	EFO:1000294
inflammatory breast carcinoma	3	MONDO:0006804	EFO:1000984
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
gastric neoplasm	2	MONDO:0021085	MONDO:0001056
plasma cell myeloma	2	MONDO:0009693	EFO:0001378
salivary gland cancer	2	MONDO:0004669	MONDO:0004669
endometrium neoplasm	1	MONDO:0021251	MONDO:0011962

4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 115.

Phase distribution

Phase	Trials
PHASE2	46
PHASE3	27
PHASE1	17
PHASE1/PHASE2	11
Not specified	9
PHASE2/PHASE3	3
PHASE4	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02658734	PHASE4	COMPLETED	A Study of Trastuzumab Emtansine in Indian Patients With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Unresectable Locally Advanced or Metastatic Breast Cancer Who Have Received Prior Treatment With Trastuzumab and a Taxane
NCT03529110	PHASE3	ACTIVE_NOT_RECRUITING	DS-8201a Versus T-DM1 for Human Epidermal Growth Factor Receptor 2 (HER2)-Positive, Unresectable and/or Metastatic Breast Cancer Previously Treated With Trastuzumab and Taxane [DESTINY-Breast03]
NCT03975647	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Tucatinib vs. Placebo in Combination With Ado-trastuzumab Emtansine (T-DM1) for Patients With Advanced or Metastatic HER2+ Breast Cancer
NCT04457596	PHASE3	ACTIVE_NOT_RECRUITING	T-DM1 and Tucatinib Compared With T-DM1 Alone in Preventing Relapses in People With High Risk HER2-Positive Breast Cancer, the CompassHER2 RD Trial
NCT04622319	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Trastuzumab Deruxtecan (T-DXd) Versus Trastuzumab Emtansine (T-DM1) in High-risk HER2-positive Participants With Residual Invasive Breast Cancer Following Neoadjuvant Therapy (DESTINY-Breast05)
NCT04873362	PHASE3	ACTIVE_NOT_RECRUITING	A Study Evaluating the Efficacy and Safety of Adjuvant Atezolizumab or Placebo and Trastuzumab Emtansine for Participants With HER2-Positive Breast Cancer at High Risk of Recurrence Following Preoperative Therapy
NCT05288777	PHASE2/PHASE3	RECRUITING	Adjuvant Chemoradiation and Biomarkers of Response in High-risk Breast Cancer
NCT06126640	PHASE3	RECRUITING	A Phase III, Active-Controlled Study of SHR-A1811 Versus Trastuzumab Emtansine (T-DM1) in HER2-Positive Primary Breast Cancer Participants With Residual Invasive Disease Following Neoadjuvant Therapy
NCT06265428	PHASE3	ACTIVE_NOT_RECRUITING	A Study to Compare DB-1303/BNT323 Versus T-DM1 in Breast Cancer
NCT06313086	PHASE3	RECRUITING	DP303c Versus Trastuzumab Emtansine in in Patients With HER2-positive Advanced Breast Cancer
NCT06316531	PHASE3	ACTIVE_NOT_RECRUITING	A Study Comparing BL-M07D1 With T-DM1 in Patients With Unresectable Locally Advanced or Metastatic HER2-positive Breast Cancer
NCT06830889	PHASE3	RECRUITING	A Study of BL-M07D1 Versus T-DM1 in the Adjuvant Treatment of HER2-positive Breast Cancer With Residual Invasive Cancer After Neoadjuvant Therapy
NCT06846437	PHASE3	RECRUITING	JSKN003 Versus Trastuzumab Emtansine (T-DM1) for HER2-Positive, Advanced Breast Cancer
NCT06968585	PHASE3	ACTIVE_NOT_RECRUITING	A Study of A166 Versus Trastuzumab Emtansine (T-DM1) in Patients With HER2-Positive Unresectable or Metastatic Breast Cancer Previously Treated With Trastuzumab and Taxane Therapy
NCT07008976	PHASE3	RECRUITING	Clinical Trial of TQB2102 for Injection Versus Trastuzumab Emtansine for Injection in HER2-positive Advanced Breast Cancer
NCT07578116	PHASE3	NOT_YET_RECRUITING	Adding Surgery and Radiation to the Usual Treatment for HER2-Positive Breast Cancer That Had Already Spread at Diagnosis
NCT00829166	PHASE3	COMPLETED	A Study of Trastuzumab Emtansine Versus Capecitabine + Lapatinib in Participants With HER2-positive Locally Advanced or Metastatic Breast Cancer
NCT01120184	PHASE3	COMPLETED	A Study of Trastuzumab Emtansine (T-DM1) Plus Pertuzumab/Pertuzumab Placebo Versus Trastuzumab [Herceptin] Plus a Taxane in Participants With Metastatic Breast Cancer (MARIANNE)
NCT01419197	PHASE3	COMPLETED	A Study of Trastuzumab Emtansine in Comparison With Treatment of Physician’s Choice in Participants With HER2-positive Breast Cancer Who Have Received at Least Two Prior Regimens of HER2-directed Therapy
NCT01641939	PHASE2/PHASE3	TERMINATED	A Study of Trastuzumab Emtansine Versus Taxane in Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Advanced Gastric Cancer
NCT01702571	PHASE3	COMPLETED	A Study of Trastuzumab Emtansine in Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Breast Cancer Who Have Received Prior Anti-HER2 And Chemotherapy-based Treatment
NCT01772472	PHASE3	COMPLETED	A Study of Trastuzumab Emtansine Versus Trastuzumab as Adjuvant Therapy in Patients With HER2-Positive Breast Cancer Who Have Residual Tumor in the Breast or Axillary Lymph Nodes Following Preoperative Therapy (KATHERINE)
NCT01966471	PHASE3	COMPLETED	A Study of Trastuzumab Emtansine (Kadcyla) Plus Pertuzumab (Perjeta) Following Anthracyclines in Comparison With Trastuzumab (Herceptin) Plus Pertuzumab and a Taxane Following Anthracyclines as Adjuvant Therapy in Participants With Operable HER2-Positive Primary Breast Cancer
NCT02131064	PHASE3	COMPLETED	A Study Evaluating Trastuzumab Emtansine Plus Pertuzumab Compared With Chemotherapy Plus Trastuzumab and Pertuzumab for Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Breast Cancer
NCT02144012	PHASE3	TERMINATED	A Study to Evaluate the Efficacy and Safety of Trastuzumab Emtansine Versus the Combination of Trastuzumab Plus Docetaxel in Patients With HER2-positive Breast Cancer
NCT03084939	PHASE3	COMPLETED	Efficacy and Safety of Trastuzumab Emtansine in Chinese Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Locally Advanced or Metastatic Breast Cancer
NCT03726879	PHASE3	COMPLETED	A Study To Evaluate the Efficacy and Safety Of Atezolizumab or Placebo in Combination With Neoadjuvant Doxorubicin + Cyclophosphamide Followed By Paclitaxel + Trastuzumab + Pertuzumab In Early Her2-Positive Breast Cancer
NCT04740918	PHASE3	TERMINATED	A Study of Trastuzumab Emtansine in Combination With Atezolizumab or Placebo as a Treatment for Participants With Human Epidermal Growth Factor 2 (HER2)-Positive and Programmed Death-ligand 1 (PD-L1)-Positive Locally Advanced (LABC) or Metastatic Breast Cancer (MBC)
NCT04924699	PHASE2/PHASE3	UNKNOWN	A Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Breast Cancer
NCT05415215	PHASE3	COMPLETED	A Study to Evaluate Patient Preference for Home Administration of Fixed-Dose Combination of Pertuzumab and Trastuzumab for Subcutaneous Administration in Participants With Early or Locally Advanced/Inflammatory HER2-Positive Breast Cancer
NCT05429684	PHASE3	UNKNOWN	Precise Therapy for Refractory HER2 Positive Advanced Breast Cancer
NCT00781612	PHASE2	ACTIVE_NOT_RECRUITING	A Safety Extension Study of Trastuzumab Emtansine in Participants Previously Treated With Trastuzumab Emtansine Alone or in Combination With Other Anti-Cancer Therapy in One of the Parent Studies
NCT01042379	PHASE2	RECRUITING	I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer
NCT02326974	PHASE2	ACTIVE_NOT_RECRUITING	T-DM1+Pertuzumab in Pre-OP Early-Stage HER2+ BRCA
NCT02465060	PHASE2	ACTIVE_NOT_RECRUITING	Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
NCT02675829	PHASE2	ACTIVE_NOT_RECRUITING	Trial of Ado-Trastuzumab Emtansine for Patients With HER2 Amplified or Mutant Cancers
NCT03587740	PHASE2	ACTIVE_NOT_RECRUITING	ATOP TRIAL: T-DM1 in HER2 Positive Breast Cancer
NCT04266249	PHASE2	ACTIVE_NOT_RECRUITING	CompassHER2-pCR: Decreasing Chemotherapy for Breast Cancer Patients After Pre-surgery Chemo and Targeted Therapy
NCT04301375	PHASE2	NOT_YET_RECRUITING	Omission of Surgery and Sentinel Lymph Node Dissection in Clinically Low-risk HER2positive Breast Cancer With High HER2 Addiction and a Complete Response Following Standard Anti- HER2-based Neoadjuvant Therapy (ELPIS Trial)
NCT04341181	PHASE2	RECRUITING	ProTarget - A Danish Nationwide Clinical Trial on Targeted Cancer Treatment Based on Genomic Profiling

Clinical evidence (CIViC)

Variant × indication × effect (16 predictive associations from 19 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
ERBB2 Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Trastuzumab Emtansine	CIViC B	EID1159 +3
ERBB2 Amplification	Colorectal Cancer	Sensitivity/Response	Trastuzumab Emtansine	CIViC B	EID7585
ERBB2 Amplification	Salivary Gland Cancer	Sensitivity/Response	Trastuzumab Emtansine	CIViC B	EID7856
ERBB2 Exon 20 Insertion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Emtansine	CIViC B	EID7683
ERBB2 Overexpression	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Trastuzumab Emtansine	CIViC B	EID4840
ERBB3 Overexpression	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab Emtansine	CIViC B	EID8707
PIK3CA Mutation	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab Emtansine	CIViC B	EID8536
PTEN Loss	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab Emtansine	CIViC B	EID8706
ERBB2 Y772_A775DUP	Lung Adenocarcinoma	Sensitivity/Response	Trastuzumab Emtansine	CIViC C	EID1125
ERBB2 V777L	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab + Trastuzumab Emtansine	CIViC C	EID5817
ERBB2 Amplification	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Emtansine	CIViC D	EID1050
PIK3CA C420R	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab Emtansine	CIViC D	EID2346
PIK3CA E545K	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab Emtansine	CIViC D	EID2036
PIK3CA H1047R	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab Emtansine	CIViC D	EID2103
PIK3CA I391M	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab Emtansine	CIViC D	EID2867
PIK3CA K111N	Her2-receptor Positive Breast Cancer	Resistance	Trastuzumab Emtansine	CIViC D	EID2866

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).