Drug · Small Molecule

Afatinib

CI-DRUG-00000043Explore in graph →NCIt C66940 CHEMBL1173655 CIViC Approved

Regulatory

Approvals (20)

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

openfdaRegulatory7 approval records · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
US FDA	—	Efficacy supplement 2022-04-07 (see label)	approved	Apr 7, 2022	openfda
US FDA	—	Efficacy supplement 2018-01-12 (see label)	approved	Jan 12, 2018

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 4	19	10	17	146	20	CA, EU, US	Jul 12, 2013	2003-11
Malignant Lung Neoplasm	Approved	Phase 4	4	1	11	50	3	EU, US	Jul 12, 2013	2007-08
Multiple Myeloma	Phase2	Phase 2	3	0	0	4	0	—	—	Aug 12, 2015
Non-Hodgkin Lymphoma	Phase2	Phase 2	3	0	0	4	0	—

Curated evidence

Clinical evidence (132)

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

civicCuratedShowing 101–132 of 132 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 T798I1
Afatinib	Malignant Breast Neoplasm

Clinical trials

Trials with this intervention (163)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 51–100 of 163 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
NCT02183883	Deciphering Afatinib Response and Resistance With INtratumour Heterogeneity(DARWIN1)	completed	Phase 2	12	University College, LondonOTHER	1	Nov 29, 2023	clinicaltrials
NCT03088059	Biomarker-based Study in R/M SCCHN(UPSTREAM)	unknown

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: V1T5K7RZ0B
Aliases: (2e)-N-(4-(3-Chloro-4-Fluoroanilino)-7-(((3s)-Oxolan-3-yl)Oxy)Quinoxazolin-6-yl)-4-(Dimethylamino)But-2-Enamide, Afatinib, AFATINIB (BIBW2992), Afatinib Dimaleate, AFATINIB DIMALEATE, AFATINIB FREE BASE, BIBW 2992, BIBW-2992, BIBW2992, BIBW2992 (AFATINIB), BIBW2992AFATINIBTOVOKS1011, BIBW2992-MA2, (E/Z)-AFATINIB, (E/Z)-BIBW 2992, GILOTRIF, Giotrif, GIOTRIF, MAR-AFATINIB, NSC-750691, SANDOZ AFATINIB, TEVA-AFATINIB, TOMTOVOK, TOVOK

Data updated 29 minutes agoSource updated unknown

Identifiers

Codes (27)

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

System	Code	Label
ATC (WHO)	L01EB03	AFATINIB
ATC (WHO)	L01XE13

ERBB2 V777L2
Afatinib	Malignant Breast Neoplasm	Predictive	C	Supports Sensitivity Response	1	accepted	EID11690 In this phase II NCI-MATCH trial, a patient with ER+ invasive ductal breast cancer with ERBB2 V777L mutation was treated with afatinib. A RECIST response was reported in the patient, however, it wasn'… (full text at CIViC) PMID 35939768 · Bedard et al., 2022 · 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

ERBB2 Amplification5
Afatinib	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	accepted	EID7807 Afatinib monotherapy was tested in patient-derived colorectal cancer (M051) mouse xenografts and gastric cancer cell-line (NCI-N87) mouse xenografts. Tumor shrinkage was observed and tumor volume was… (full text at CIViC) PMID 26296355 · Leto et al., 2015 · Open in CIViC	civic
〃	Malignant Gastric Neoplasm	Predictive	D	Supports Sensitivity Response	3	submitted	EID7808 Afatinib monotherapy was tested in patient-derived colorectal cancer (M051) mouse xenografts and gastric cancer cell-line (NCI-N87) mouse xenografts. Tumor shrinkage was observed and tumor volume was … (full text at CIViC) PMID 26296355 · Leto et al., 2015 · Open in CIViC	civic
〃	Pancreatic Adenocarcinoma	Predictive	D	Supports Sensitivity Response	2	accepted	EID962 Afatinib was growth-inhibitory for three pancreatic cancer cell lines but cytotoxic only toward BxPC3 (KRAS wt) and Capan-2 (KRAS mut) cells, both of which express high levels of EGFR, ERBB2, and ERBB… (full text at CIViC) PMID 26668065 · Huguet et al., 2016 · Open in CIViC	civic
〃	Transitional Cell Carcinoma	Predictive	B	Supports Sensitivity Response	2	submitted	EID7810 In this phase II trial, patients with metastatic platinum-refractory urothelial carcinoma (UC) received afatinib (40 mg/day). Among the 21 tumors, five of six patients (83.3%) with ERBB2 (HER2) and/or… (full text at CIViC) PMID 27044931 · Choudhury et al., 2016 · Open in CIViC	civic
〃	Uterine Corpus Endometrial CarcinomaUNRESOLVED	Predictive	D	Supports Sensitivity Response	2	accepted	EID886 Eight uterine cancer cell lines (four with ERBB2 amplification and four without) were treated with scalar concentrations of afatinib. Primary chemotherapy-resistant USC cell lines harbouring ERBB2 gen… (full text at CIViC) PMID 25268372 · Schwab et al., 2014 · Open in CIViC	civic

NRG1 Fusion2
Afatinib	Mucinous Adenocarcinoma	Predictive	C	Supports Sensitivity Response	3	submitted	EID7490 A 62 year old nonsmoker with KRAS and ERBB family wild-type metastatic pulmonary adenocarcinoma was found to have a CD74-NRG1 fusion. The patient achieved a durable response when treated with afatinib… (full text at CIViC) PMID 28502724 · Gay et al., 2017 · Open in CIViC	civic
〃	Mucinous Adenocarcinoma	Predictive	C	Supports Sensitivity Response	3	submitted	EID7494 A single case of pulmonary mucinous adenocarcinoma in a 62 year old patient was found to have a CD74-NRG1 fusion. Afatinib treatment resulted in symptomatic and radiographic response for 26 weeks, at … (full text at CIViC) PMID 29169524 · Cheema et al., 2017 · Open in CIViC	civic

NRG1 Fusion2
Afatinib	Pancreatic Adenocarcinoma	Predictive	C	Supports Sensitivity Response	4	accepted	EID6273 In patients with KRAS wild-type (KRASwt) tumors druggable gene fusions have been identified. These alterations included recurrent NRG1 rearrangements predicted to drive PDAC development through aberra… (full text at CIViC) PMID 29802158 · Heining et al., 2018 · Open in CIViC	civic
〃	Mucinous Lung AdenocarcinomaUNRESOLVED	Predictive	C	Does Not Support Sensitivity Response	3	accepted	EID6096 One patient with an NRG1-rearranged invasive mucinous adenocarcinomas (IMAs) of the lung had a response with an anti-ERBB3 monoclonal antibody (GSK2849330). No response was achieved with afatinib in f… (full text at CIViC) PMID 29610121 · Drilon et al., 2018 · Open in CIViC	civic