Drug · Small Molecule

Neratinib

CI-DRUG-00000402Explore in graph →NCIt C49094 CHEMBL180022 CIViC Approved

Regulatory

Approvals (9)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

health-canada-dpdRegulatory9 approval records from 3 sources (hover a row badge for its dataset) · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
CA Health Canada	—	Marketed in Canada as NERLYNX (DIN 02490536) under ATC L01EH02 NERATINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Dec 20, 2019	health-canada-dpd
EU

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 2 days agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 3	19	14	3	66	9	CA, EU, US	Jul 17, 2017	2003-11
Malignant Breast Neoplasm	Approved	Phase 3	10	8	1	34	3	EU, US	Jul 17, 2017	Apr 4, 2007
Malignant Ovarian Neoplasm	Phase2	Phase 2	2	1	0	2	0	—	—	Aug 24, 2020
Leukemia	Phase2	Phase 2	1	0	0	2	0	—

Curated evidence

Clinical evidence (43)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–43 of 43 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
ERBB2 Amplification8
Neratinib	HER2-Positive Breast Carcinoma

Clinical trials

Trials with this intervention (71)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–50 of 71 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT05564377	Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial	recruiting	Phase 2	2,900	National Cancer Institute (NCI)NIH	2	Sep 29, 2026	clinicaltrials
NCT07152782	T-DXd With or Without Neratinib for HER2 Positive Breast Cancer With Brain Metastasis(THUNDER)

Molecule

Record

Kind: Small Molecule
Mechanism: Epidermal growth factor receptor erbB1 inhibitor; Receptor protein-tyrosine kinase erbB-2 inhibitor; Receptor protein-tyrosine kinase erbB-4 inhibitor
Targets: 3 genes
UNII: 9RM7XY23ZS
Aliases: 2-Butenamide, N-(4-((3-chloro-4-(2-pyridinylmethoxy)phenyl)amino)-3-cyano-7-ethoxy-6-quinolinyl)-4-(dimethylamino)-, (2E)-, (2E)-N-(4-((3-chloro-4-((pyridin-2-yl)methoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide, CDP-820, HKI 272, HKI-272, HKI272, Neratinib, Neratinib Maleate, NERLYNX, PB 272, WAY-179272

Data updated 1 hour agoSource updated unknown

Identifiers

Codes (4)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EH02	NERATINIB
DIN (Health Canada)	02490536

ERBB2 G292R2
Neratinib	Malignant Bladder NeoplasmALIAS	Predictive	B	Does Not Support Sensitivity Response	2	accepted	EID12119 In the SUMMIT basket trial (clinicaltrials.gov identifier NCT01953926) patients with solid tumors of various histologies harboring mutations of either HER2 or HER3 were enrolled and treated with the p… (full text at CIViC) PMID 29420467 · Hyman et al., 2018 · Open in CIViC	civic
Afatinib + Lapatinib + Neratinib + Osimertinib + TrastuzumabSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID12116 A sequencing-based method was used to assess the sensitivity of this variant relative to wild-type to trastuzumab, lapatinib, sapatinib, afatinib, neratinib and osimertinib. Results indicated sensitiv… (full text at CIViC) PMID 29967253 · Nagano et al., 2018 · Open in CIViC	civic

ERBB2 Amplification + YES1 AmplificationERBB2 YES12
Neratinib	Malignant Breast Neoplasm	Predictive	D	Supports Resistance	3	submitted	EID12095 Neratinib-resistant cell lines were established by stepwise escalation method and high concentration method in breast cancer cell line BT-474 and lung cancer cell line H2170 with HER2 amplification. E… (full text at CIViC) PMID 31856375 · Takeda et al., 2020 · Open in CIViC	civic
〃	Malignant Lung Neoplasm	Predictive	D	Supports Resistance	3	submitted	EID12096 Neratinib-resistant cell lines were established by stepwise escalation method and high concentration method in breast cancer cell line BT-474 and lung cancer cell line H2170 with HER2 amplification. E… (full text at CIViC) PMID 31856375 · Takeda et al., 2020 · Open in CIViC	civic

ERBB2 L755S3
Neratinib	Malignant Breast Neoplasm	Predictive	D	Supports Sensitivity Response	5	accepted	EID283 The L755S mutation showed mild response to neratinib in MCF10A cell lines retrovirally transduced with wildtype or mutant ERBB2. PMID 23220880 · Bose et al., 2013 · Open in CIViC	civic
Lapatinib + Neratinib + TrastuzumabCombination	Malignant Colon Neoplasm	Predictive	D	Supports Sensitivity Response	4	accepted	EID1176 Colon cancer patient derived xenografts with HER2 mutations are sensitive to HER2 targeted drugs and the greatest tumor reduction was seen with the combination of a tyrosine kinase inhibitor with tras… (full text at CIViC) PMID 26243863 · Kavuri et al., 2015 · Open in CIViC	civic
Capecitabine + NeratinibCombination	Triple-Negative Breast CarcinomaALIAS	Predictive	C	Supports Sensitivity Response	2	submitted	EID8055 This patient originally presented in the clinic with an ER+, PR-, and HER2- mass on the left breast and bone metastasis. Family history showed negative germline mutations in BRCA1/2. Patient responded… (full text at CIViC) PMID 26358790 · Ben-Baruch et al., 2015 · Open in CIViC	civic

ERBB2 V777L5
Neratinib	Malignant Breast Neoplasm	Predictive	D	Supports Sensitivity Response	5	accepted	EID288 In MCF10A cell lines, the V777L mutation was shown to be sensitive to neratinib. PMID 23220880 · Bose et al., 2013 · Open in CIViC	civic
Lapatinib + Neratinib + TrastuzumabCombination	Malignant Colon Neoplasm	Predictive	D	Supports Sensitivity Response	4	accepted	EID1177 Colon cancer patient derived xenografts with HER2 mutations are sensitive to HER2 targeted drugs and the greatest tumor reduction was seen with the combination of a tyrosine kinase inhibitor with tras… (full text at CIViC) PMID 26243863 · Kavuri et al., 2015 · Open in CIViC	civic
Neratinib	Malignant NeoplasmALIAS	Predictive	B	Does Not Support Sensitivity Response	3	submitted	EID12106 In the SUMMIT basket trial (NCT01953926) patients with solid tumors of various histologies harboring mutations of either HER2 or HER3 were enrolled and treated with the pan-HER kinase inhibitor nerati… (full text at CIViC) PMID 29420467 · Hyman et al., 2018 · Open in CIViC	civic
Afatinib + Lapatinib + Neratinib + OsimertinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID12101 Ba/F3 mouse lymphoid cells expressing wild-type or V777L mutant HER2 were treated with afatinib, neratinib, osimertinib or DMSO (vehicle) for 72 hours, at which time viable cells were measured using t… (full text at CIViC) PMID 29967253 · Nagano et al., 2018 · Open in CIViC	civic
Neratinib	Pancreatic Ductal Adenocarcinoma	Predictive	D	Supports Sensitivity Response	3	submitted	EID11569 Neratinib suppresses anchorage-independent growth in transduced HPNE cells with the variant in a concentration-dependent manner (Figure 6B–C) with complete inhibition at a concentration of 0.5 µM (Fig… (full text at CIViC) PMID 31046123 · Li et al., 2020 · Open in CIViC	civic

ERBB2 V842I2
Neratinib	Malignant Breast Neoplasm	Predictive	D	Supports Sensitivity Response	5	accepted	EID289 In MCF10A cell lines, the V842I mutation was shown to be sensitive to neratinib. PMID 23220880 · Bose et al., 2013 · Open in CIViC	civic
Lapatinib + Neratinib + TrastuzumabCombination	Malignant Colon Neoplasm	Predictive	D	Supports Sensitivity Response	4	accepted	EID1174 Colon cancer patient derived xenografts with HER2 mutations are sensitive to HER2 targeted drugs and the greatest tumor reduction was seen with the combination of a tyrosine kinase inhibitor with tras… (full text at CIViC) PMID 26243863 · Kavuri et al., 2015 · Open in CIViC	civic