ERBB2 erb-b2 receptor tyrosine kinase 2
ENSG00000141736 · protein coding · Open Targets profile
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, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. This prevents the phosphorylation of APC and CLASP2, allowing its association with the cell membrane. In turn, membrane-bound APC allows the localization of MACF1 to the cell membrane, which is required for microtubule capture and stabilization. .
Each band is a group of drugs. It runs from the kind of drug on the left to the furthest stage that drug has reached in any disease on the right. Thicker bands mean more drugs.
Approved bands are highlighted. Withdrawn means the drug was pulled from the market or from development. A combined phase counts as the later one (Phase 1/2 is shown as Phase 2). Hover a band for the drug names. Source: Open Targets Platform, fetched live.
Each row is a cancer, strongest overall evidence first. The two dots show how strong the inherited (germline) and tumour-mutation (somatic) evidence is; the line between them is the gap.
Scores run from 0 (no evidence) to 1 (strongest). A missing dot at 0 means Open Targets holds no evidence of that kind. Source: Open Targets Platform, fetched live.
Tractability
- Small molecule
- Approved Drug, Structure with Ligand, High-Quality Ligand, High-Quality Pocket, Druggable Family
- Antibody
- Approved Drug, UniProt loc high conf, GO CC high conf, UniProt SigP or TMHMM, Human Protein Atlas loc
- PROTAC
- Literature, Database Ubiquitination, Half-life Data, Small Molecule Binder
- Other modalities
- Approved Drug
gnomAD loss of function constraint: o/e 0.40928998589515686 (upper bound 0.5065400004386902). Low values mean loss of function is poorly tolerated, a safety flag for inhibition.
Who runs trials of these drugs
Principal investigators and study chairs on 400 registry trials, updated in the last three years, of the most advanced drugs against ERBB2 (lapatinib, masoprocol, dacomitinib, zanidatamab, tucatinib, trastuzumab duocarmazine, neratinib, margetuximab, afatinib, zenocutuzumab, pertuzumab, trastuzumab emtansine), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.
- Adrienne WaksDana-Farber Cancer Institute · 4 of 4 trials Phase 2+
- Xingchen PengWest China Hospital · 3 of 5 trials Phase 2+Ph1NCT06741982 · A Clinical Study on Neoadjuvant Treatment of Resectable Head and Neck Squamous Carcinoma With Immune-targeted Therapy and Lysogenic HSV Virusbrief
- Zhimin ShaoFudan University · 3 of 3 trials Phase 2+
- Joanne MortimerCity of Hope Medical Center · 2 of 3 trials Phase 2+N/ANCT02226276 · Copper Cu 64-DOTA-Trastuzumab PET in Predicting Response to Treatment With Ado-Trastuzumab Emtansine in Patients With Metastatic HER2 Positive Breast Cancerbrief
- Ajay DhakalUniversity of Rochester · 2 of 2 trials Phase 2+
- Antonio Llombart-CussacArnau de Vilanova Hospital, Valencia (Spain) · 2 of 2 trials Phase 2+
- Barbara PISTILLIGustave Roussy, VILLEJUIF · 2 of 2 trials Phase 2+
- Chau DangMemorial Sloan Kettering Cancer Center · 2 of 2 trials Phase 2+
- F OpdamThe Netherlands Cancer Institute · 2 of 2 trials Phase 2+
- François-Clément BidardInstitut Curie · 2 of 2 trials Phase 2+
- Herui YaoSun Yat-Sen Memorial Hospital of Sun Yat-Sen University · 2 of 2 trials Phase 2+
- Julien EdelineCentre Eugène Marquis · 2 of 2 trials Phase 2+
- Matthew KrebsThe Christie Hospital · 2 of 2 trials Phase 2+
- Rachel FreedmanDana-Farber Cancer Institute · 2 of 2 trials Phase 2+
- Rachel LaymanM.D. Anderson Cancer Center · 2 of 2 trials Phase 2+
Registry trials of lapatinib, masoprocol, dacomitinib, zanidatamab, tucatinib, trastuzumab duocarmazine, neratinib, margetuximab, afatinib, zenocutuzumab, pertuzumab, trastuzumab emtansine updated in the last three years, counted by the country group of their listed sites. A trial with sites in several groups counts in each; 263 of 362 have all sites in one country.
Site counts are not patients per country, and trials registered only outside ClinicalTrials.gov are not covered. Where sites are is a fact about the record, not a judgement of its quality. Europe is the EU and EEA, the UK and Switzerland. 38 trials list no sites and are left out. Source: ClinicalTrials.gov, fetched live.
192 trials of drugs against ERBB2 were stopped early; 21 give no reason
Terminated, withdrawn and suspended interventional trials of lapatinib, masoprocol, dacomitinib, zanidatamab, tucatinib, trastuzumab duocarmazine, neratinib, margetuximab, afatinib, zenocutuzumab, pertuzumab, trastuzumab emtansine, newest update first, live from ClinicalTrials.gov. Each reason is quoted exactly as the registry gives it; we do not sort reasons into safety, efficacy or business. Dates are the last registry update. Showing the 25 most recent of 192.
- suspended · 2026-10-21 · Virginia Commonwealth University · Neratinib“Pending amendment approval”
- withdrawn · 2026-10-16 · West China Hospital · Afatinib“The study was withdrawn prior to participant enrollment due to administrative and protocol optimization considerations.”
- terminated · 2026-09-30 · Breast Cancer Trials, Australia and New Zealand · Tucatinib“Stopped on the recommendation of the BCT Independent Data and Monitoring Committee”
- terminated · 2026-08-20 · Jules Bordet Institute · Trastuzumab emtansine“Study logistics or limited study population, as defined by the iclusion/exclusion criteria, leading to a poor recruitment”
- terminated · 2026-07-22 · M.D. Anderson Cancer Center · Neratinib“<75% participation”
- terminated · 2026-06-03 · Petrov, Andrey · Afatinib Dimaleat, inhalation of afatinib dimaleate“adjustment of the study design taking into account the receipt of primary data”
- terminated · 2026-05-29 · National Cancer Institute (NCI) · Pertuzumab“Inadequate accrual rate”
- terminated · 2026-04-27 · Partner Therapeutics, Inc. · Afatinib Oral Tablet“Merus terminated the study early due to changes in organizational priorities.”
- terminated · 2026-04-21 · Institut Paoli-Calmettes · BKM120 + lapatinib“Drug development withdrawn”
- terminated · 2026-04-02 · Spanish Breast Cancer Research Group · matched by the registry's drug synonyms“The study stopped due to insufficient accrual (only two patients were included), and the sponsor has decided on its premature termination.”
- terminated · 2026-03-13 · Biocon Biologics UK Ltd · matched by the registry's drug synonyms“US FDA is streamlining the Biosimilar development. Thus, Biocon decided to terminate the study.”
- terminated · 2026-02-12 · M.D. Anderson Cancer Center · Neratinib, Pertuzumab“<75% accrued”
- suspended · 2026-02-03 · Gruppo Oncologico del Nord-Ovest · Tucatinib“due to earlier termination of the agreement between the Sponsor and Central Laboratory for screening test. Enrollment will reopen as soon as a new laboratory is identified.”
- terminated · 2026-01-22 · Dana-Farber Cancer Institute · Neratinib“Slow accrual”
- terminated · 2026-01-06 · Fundacio Clinic Barcelona · Trastuzumab and pertuzumab Subcutaneous Fixed-Dose Combination“The study was prematurely halted primarily due to low patient accrual. Despite efforts to optimize recruitment, the enrollment rate remained insufficient to meet the predefined targets, and continuation was deemed unfeasible”
- terminated · 2025-12-31 · Baptist Health South Florida · Combined use of SRS with Tucatinib, Trastuzumab, and Capecitabine“Slow enrollment”
- terminated · 2025-12-10 · Spanish Breast Cancer Research Group · Tucatinib“The study was closed early due to safety concerns and an unfavorable benefit-risk balance. Unexpected high neutropenia rates required a costly sub-study, which was not feasible, forcing the sponsor to terminate the trial prematurely.”
- withdrawn · 2025-12-02 · Beijing Bio-Targeting Therapeutics Technology Co., Ltd · matched by the registry's drug synonyms“The applicant voluntarily withdrew the case”
- terminated · 2025-12-01 · Gustave Roussy, Cancer Campus, Grand Paris · Pertuzumab“Abandon of the partner, ROCHE”
- terminated · 2025-11-20 · Bolt Biotherapeutics, Inc. · Pertuzumab“Sponsor Decision”
- withdrawn · 2025-11-19 · West China Hospital · Afatinib“The study was withdrawn prior to participant enrollment due to administrative and protocol optimization considerations.”
- withdrawn · 2025-10-14 · University of Rochester · Pertuzumab, Trastuzumab emtansine“Change in the landscape of current treatment of early stage breast cancer. Larger clinical trials answering similar questions are expected to result in the next few years.”
- withdrawn · 2025-10-14 · EirGenix, Inc. · matched by the registry's drug synonyms“Following SA from both the US FDA and the EMA, EirGenix, Inc. has decided to streamline the clinical-development program for EG1206A (biosimilar to Perjeta). EirGenix has concluded that the continuation of the study in no longer necessary.”
- terminated · 2025-10-09 · University of Southern California · lapatinib ditosylate“Trial not progressing toward scientific goals”
- terminated · 2025-10-01 · National Cancer Institute (NCI) · Pertuzumab“Inadequate accrual rate”
Paediatric incentives and obligations for ERBB2's drugs
For lapatinib, masoprocol, dacomitinib, zanidatamab, tucatinib, trastuzumab duocarmazine, neratinib, margetuximab, afatinib, zenocutuzumab, pertuzumab, trastuzumab emtansine: what EMA and FDA publish about paediatric plans, orphan status and pediatric approvals, and how many registered studies take children. Each line is a yes, no or not published fact from the record linked under it; none of it is a forecast.
- FDA pediatric target list: yes · ERBB2 is on the list. Membership alone neither requires nor waives a pediatric study.Rule: Target is on FDA's Pediatric Molecular Target List (relevant targets). Source: FDA Pediatric Molecular Target List (Listed as February 2026 on the FDA Pediatric Oncology page; the file served is 9.7.22_the_relevant_molecular_target_list.xlsx, whose Summary of Changes sheet is headed 'SEPTEMBER 2022 UPDATE' (footnote date 2022-09-01)), 2026-11-11
- EU paediatric investigation plan: yes · EMEA-003519-PIP01-23 (zenocutuzumab, Treatment of lung cancer;Treatment of pancreatic cancer): W: decision granting a waiver in all age groups for all conditions or indications, 7 Mar 2024; EMEA-003450-PIP01-23 (zanidatamab, Treatment of biliary tract cancer): W: decision granting a waiver in all age groups for all conditions or indications, 27 Oct 2023; EMEA-002242-PIP02-21 (tucatinib, Treatment of solid tumours): W: decision granting a waiver in all age groups for all conditions or indications, 11 Mar 2022; EMEA-001596-PIP02-17-M02 (afatinib, Treatment of all conditions included in the category of malignant neoplasms (excluding central nervous system, haematopoietic and lymphoid tissue neoplasms);Treatment of malignant neoplasms of the central nervous system): PM: decision on the application for modification of an agreed PIP, 13 May 2020; compliance positive 23 Apr 2021; +2 moreRule: An EMA PIP decision (agreement, modification or waiver) lists the drug as its active substance, exact name. Source: EMA data download (dated snapshot), 2026-11-11
- EU orphan designation: yes · EU/3/25/3155 positive 21 Nov 2025: Treatment of oesophageal cancer; EU/3/21/2458 positive 27 Jun 2025: Treatment of biliary tract cancer; EU/3/21/2458 positive 19 Jul 2021: Treatment of biliary tract cancer; EU/3/24/2929 positive 28 Jun 2024: Treatment of complex regional pain syndrome; +2 moreRule: An EU orphan designation lists the drug as its active substance (exact name) or belongs to a medicine that does; withdrawn and expired designations are listed with their status. Source: EMA data download (dated snapshot), 2026-11-11
- Authorised in the EU: yes · Phesgo: authorised since 21 Dec 2020; Vizimpro: authorised since 2 Apr 2019; Poherdy: authorised since 23 Apr 2026; Pebrilzo: opinion; +8 moreRule: An EMA medicine record lists the drug as its active substance or INN, exact name; national-only authorisations are not in this file. Source: EMA data download (dated snapshot), 2026-11-11
- FDA orphan designation: not published · FDA's orphan designation database turns away automated requests, so this app does not read it; search it by hand at the linkRule: Would be: an FDA orphan designation names the drug. Source: FDA orphan designations search
- FDA pediatric oncology approval: no · FDA's table lists no pediatric approval of lapatinib, masoprocol, dacomitinib, zanidatamab, tucatinib, trastuzumab duocarmazine, neratinib, margetuximab, afatinib, zenocutuzumab, pertuzumab, trastuzumab emtansineRule: FDA's Pediatric Oncology Drug Approvals table names the drug. Source: FDA Pediatric Oncology Drug Approvals (content current as of 2026-03-03), 2026-11-11
- Registered studies open to children: yes · 30 interventional studies of lapatinib, masoprocol, dacomitinib, zanidatamab, tucatinib, trastuzumab duocarmazine, neratinib, margetuximab, afatinib, zenocutuzumab, pertuzumab, trastuzumab emtansine include patients under 18; 11 are recruiting, not yet recruiting or activeRule: The registry's age group includes Child (birth to 17 years), which also counts studies that set no minimum age. Source: ClinicalTrials.gov search, 2026-11-11
Rare pediatric disease voucher. FDA, content current as of 29 Apr 2026: “As of February 3, 2026, enactment of the Consolidated Appropriations Act, 2026, the rare pediatric disease PRV program will sunset after September 30, 2029. FDA may not award any PRVs under this program after September 30, 2029.” Voucher sale prices are not shown here; they appear only as company-reported news. FDA: Rare Pediatric Disease Designation and Priority Review Voucher Programs
All 48 drugs and clinical candidates as a table
Each drug, stage and indication links to its Open Targets record, where the trials and approvals behind it are listed. Salt forms (for example a mesylate) are listed as Open Targets records them, as separate entries.