Patritumab Deruxtecan

Summary

Patritumab Deruxtecan (CHEMBL4594611) is a phase-3 clinical-stage antibody drug conjugate (ATC L01FX36) targeting ERBB3; indicated across 4 conditions including neoplasm and non-small cell lung carcinoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Antibody drug conjugate
• ATC class: L01FX36
• Targets: 1 (ERBB3)
• Indications: 4 conditions
• Clinical trials: 18

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4594611
Name	Patritumab Deruxtecan
Type	Antibody drug conjugate
Max phase	3
ATC	L01FX36

Also known as: Patritumab deruxtecan, U3 1402, U31402, PATRITUMAB DERUXTECAN

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
ERBB3	erb-b2 receptor tyrosine kinase 3	Binding	9	7.9%	P21860

Bioactivity

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

Target pathways

Aggregated over 1 target gene(s): ERBB3.

Top Reactome pathways

15 total, by targets touching each:

Pathway	Targets	Genes
Signaling by ERBB2	1	ERBB3
Signaling by ERBB4	1	ERBB3
SHC1 events in ERBB2 signaling	1	ERBB3
PIP3 activates AKT signaling	1	ERBB3
GRB7 events in ERBB2 signaling	1	ERBB3
Downregulation of ERBB2:ERBB3 signaling	1	ERBB3
PI3K events in ERBB2 signaling	1	ERBB3
Constitutive Signaling by Aberrant PI3K in Cancer	1	ERBB3
RAF/MAP kinase cascade	1	ERBB3
ERBB2 Regulates Cell Motility	1	ERBB3
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	1	ERBB3
ERBB2 Activates PTK6 Signaling	1	ERBB3
Downregulation of ERBB2 signaling	1	ERBB3
Signaling by ERBB2 KD Mutants	1	ERBB3
Signaling by ERBB2 TMD/JMD mutants	1	ERBB3

Dominant GO biological processes

GO term	Targets
endocardial cushion development	1
negative regulation of cell adhesion	1
signal transduction	1
cell surface receptor protein tyrosine kinase signaling pathway	1
epidermal growth factor receptor signaling pathway	1
peripheral nervous system development	1
heart development	1
negative regulation of signal transduction	1
positive regulation of gene expression	1
Schwann cell differentiation	1
Schwann cell development	1
cranial nerve development	1
neuron differentiation	1
ERBB2-ERBB3 signaling pathway	1
wound healing	1

Indications & clinical

Indications

4 indications (0 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
neoplasm	3	MONDO:0005070	EFO:0000616
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
breast neoplasm	2	MONDO:0021100	MONDO:0007254
breast carcinoma	2	MONDO:0004989	EFO:0000305

Clinical trials

Total trials: 18.

Phase distribution

Phase	Trials
PHASE2	8
PHASE1/PHASE2	7
PHASE3	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05338970	PHASE3	ACTIVE_NOT_RECRUITING	HERTHENA-Lung02: A Study of Patritumab Deruxtecan Versus Platinum-based Chemotherapy in Metastatic or Locally Advanced EGFRm NSCLC After Failure of EGFR TKI Therapy
NCT07060807	PHASE3	RECRUITING	A Clinical Study of Patritumab Deruxtecan to Treat Breast Cancer (MK-1022-016)
NCT04965766	PHASE2	RECRUITING	Patritumab Deruxtecan (U3-1402) in Unresectable Locally Advanced or Metastatic Breast Cancer
NCT05569811	PHASE2	ACTIVE_NOT_RECRUITING	NeoadjuVAnt muLti-agENT Chemotherapy or Patritumab Deruxtecan With or Without endocrINE Therapy for High-risk HR+/HER2- Breast Cancer - VALENTINE Trial
NCT06298084	PHASE1/PHASE2	RECRUITING	Dose-Expansion Modular Study To Explore the Safety, Tolerability, and Anti-tumor Activity of HER3- DXd Monotherapy and Combinations in Patients With Inoperable Advanced Breast Cancer (ABC) After Progression on T-DXd
NCT06383884	PHASE2	RECRUITING	Patritumab Deruxtecan in Patients With Solid Tumor Harboring an NRG1 Fusion
NCT06469944	PHASE1/PHASE2	RECRUITING	Substudy 06C: A Study of Investigational Agents With Pembrolizumab (MK-3475) and Chemotherapy in Participants With First-Line Locally Advanced Unresectable/Metastatic Gastroesophageal Adenocarcinoma (MK-3475-06C/KEYMAKER-U06)
NCT06596694	PHASE1/PHASE2	RECRUITING	Study of Patritumab Deruxtecan in Participants With Gastrointestinal Cancers (MK-1022-011) (HERTHENA-PanTumor02)
NCT06686394	PHASE1/PHASE2	RECRUITING	Study of Patritumab Deruxtecan With Other Anticancer Agents in Participants With HER2 Positive Breast Cancer That Has Spread and Cannot Be Surgically Removed (MK-1022-009)
NCT06797635	PHASE2	RECRUITING	Study of Patritumab Deruxtecan Plus Pembrolizumab With Other Anticancer Agents in Participants With High-Risk Early-Stage Triple-Negative or Hormone Receptor-Low Positive/HER-2 Negative Breast Cancer (MK-1022-010, HERTHENA-Breast-03)
NCT06941272	PHASE1/PHASE2	RECRUITING	A Study of Patritumab Deruxtecan in Pediatric Participants With Relapsed or Refractory Solid Tumors (MK-9999-01C/LIGHTBEAM-U01)
NCT07286149	PHASE1/PHASE2	RECRUITING	A Clinical Study of MK-1084 With Other Treatments for Non-small Cell Lung Cancer (MK-3475-01F)
NCT02980341	PHASE1/PHASE2	COMPLETED	Phase I/II Study of U3-1402 in Subjects With Human Epidermal Growth Factor Receptor 3 (HER3) Positive Metastatic Breast Cancer
NCT04479436	PHASE2	TERMINATED	A Study to Evaluate U3-1402 in Subjects With Advanced or Metastatic Colorectal Cancer
NCT04699630	PHASE2	COMPLETED	A Study of U3-1402 (Patritumab Deruxtecan) in Subjects With Metastatic Breast Cancer
NCT05620914	PHASE2	WITHDRAWN	A Window of Opportunity Study of Patritumab Deruxtecan in Patients With Brain Metastases
NCT05865990	PHASE2	COMPLETED	HER3-DXd in Breast Cancer and NSCLC Brain Metastases and Solid Tumor Leptomeningeal Disease
NCT04610528	EARLY_PHASE1	UNKNOWN	A Window-of-opportunity Study of U3-1402, a HER3-targeting Antibody-drug Conjugate in Operable Breast Cancer According to ERBB3 Expression

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

37 molecules share ≥1 primary target. Top 37 by shared-target count:

Molecule	Source	Status	Shared targets
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
BOSUTINIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
ERLOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
LAPATINIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
MOBOCERTINIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
NERATINIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
OSIMERTINIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
VANDETANIB	ChEMBL + PubChem	Phase 4 (approved)	ERBB3
DASATINIB	ChEMBL	Phase 4 (approved)	ERBB3
ALVOCIDIB	ChEMBL	Phase 3	ERBB3
CANERTINIB	ChEMBL	Phase 3	ERBB3
CEDIRANIB	ChEMBL	Phase 3	ERBB3
LESTAURTINIB	ChEMBL	Phase 3	ERBB3
ROCILETINIB	ChEMBL	Phase 3	ERBB3
AEE-788	ChEMBL	Phase 2	ERBB3
FORETINIB	ChEMBL	Phase 2	ERBB3
MAVELERTINIB	ChEMBL	Phase 2	ERBB3
PF-06459988	ChEMBL	Phase 2	ERBB3
SAPITINIB	ChEMBL	Phase 2	ERBB3
TOZASERTIB	ChEMBL	Phase 2	ERBB3
Acalabrutinib	PubChem	Approved	ERBB3
Axitinib	PubChem	Approved	ERBB3
Crizotinib	PubChem	Approved	ERBB3
dacomitinib	PubChem	Approved	ERBB3
Fedratinib	PubChem	Approved	ERBB3
Ibrutinib	PubChem	Approved	ERBB3
Imatinib	PubChem	Approved	ERBB3
Midostaurin	PubChem	Approved	ERBB3
Nilotinib	PubChem	Approved	ERBB3
Pazopanib	PubChem	Approved	ERBB3
Quizartinib	PubChem	Approved	ERBB3
Ruxolitinib	PubChem	Approved	ERBB3
Selumetinib	PubChem	Approved	ERBB3
Sorafenib	PubChem	Approved	ERBB3
Sunitinib	PubChem	Approved	ERBB3
Tofacitinib	PubChem	Approved	ERBB3