Nerlynx

(neratinib)

ApprovedSmall molecule

Neratinib is used to treat certain types of breast cancer, particularly HER2-positive breast cancer, either as an initial treatment or to prevent cancer from coming back after other treatments.[2] Nerlynx is currently approved and in use across 18 indications[4].[1]

Nerlynx is one of 464 small molecule programs targeting Hepatic failure. It is currently in Approved.

Indications

Total Trials

Active Trials

463

Competitors

FDA Application

NDA/BLA/ANDA regulatory filings

Patents

Pipeline

Status by Indication[4][1]

Indication

Hepatic FailureApproved

NF2-Related SchwannomatosisActive, not recruiting

Esophageal CancerActive, not recruiting

Chronic Myelogenous LeukemiaApproved

Breast NeoplasmApproved

Metastatic Colorectal CancerActive, not recruiting

HER2 Positive Breast CarcinomaApproved

Liver DiseaseActive, not recruiting

Non-Small Cell Lung CancerActive, not recruiting

Breast CancerActive, not recruiting

Hepatic FailureApproved

Approved

NF2-Related SchwannomatosisPhase 2

Active, not recruiting

Esophageal CancerPhase 2

Active, not recruiting

Chronic Myelogenous LeukemiaApproved

Approved

Breast NeoplasmApproved

Approved

Metastatic Colorectal CancerPhase 2

Active, not recruiting

HER2 Positive Breast CarcinomaApproved

Approved

Liver DiseasePhase 1

Active, not recruiting

Non-Small Cell Lung CancerPhase 2

Active, not recruiting

Breast CancerPhase 3

Active, not recruiting

Showing 10 of 18 indications

Competition

Competitive Landscape

2828 competitors in Breast Cancer

#DrugCompanyPhaseTrials

Nerlynx

PPuma Biotechnology, Inc.

Approved

33 2

Halaven

Eisai

Preclinical

38 3

Tecentriq

Roche

Preclinical

36 4

Tykerb

GSK

Preclinical

80 5

Trodelvy

Gilead

Preclinical

37 6

Adriamycin

GGynecologic Oncology Group

Preclinical

87 7

Avastin

BBio-Thera Solutions

Preclinical

153 8

Nolvadex

SSan Diego Pacific Oncology & Hematology Associates

Preclinical

78 9

Prolia

Amgen

Preclinical

14 10

Gemzar

GGynecologic Oncology Group

Preclinical

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Timeline

Expected Milestones

Q4 2026

Phase 1/2Active, not recruiting

Treatment

NCT02932280

Phase 1Recruiting

TNBC

NCT06008275

Phase 1/2Active, not recruiting

Breast Cancer

NCT03377387

Q3 2027

Phase 2Recruiting

Breast Cancer

NCT04886531

Q1 2028

Phase 2Recruiting

Pancreatic Ductal Carcinoma

NCT06813079

Q2 2028

Phase 2Recruiting

Esophageal Cancer

NCT06109467

Clinical

Trials by Indication[1]

Breast Cancer33 trials

Neratinib and Paclitaxel With or Without Pertuzumab and Trastuzumab Before Combination Chemotherapy in Treating Patients With Metastatic or Locally Advanced Breast Cancer

Terminated·MM.D. Anderson Cancer Center·Phase 1/2·NCT03101748·34 enrolled

Phase II Randomized Trial Evaluating Neoadjuvant Therapy With Neratinib and/or Trastuzumab Followed by Postoperative Trastuzumab in Women With Locally Advanced HER2-positive Breast Cancer

Completed·NNSABP Foundation Inc·Phase 2·NCT01008150·141 enrolled

Combination of Weekly Paclitaxel With Neratinib and Trastuzumab in Women With Metastatic HER2-positive Breast Cancer

Completed·NNSABP Foundation Inc·Phase 1·NCT01423123·21 enrolled

Show 30 more trials

Neoadjuvant Neratinib in Stage I-III HER2-Mutated Lobular Breast Cancers

Recruiting·VVanderbilt-Ingram Cancer Center·Phase 2·NCT05919108·30 enrolled

An Open-Label Study to Characterize the Incidence and Severity of Diarrhea in Patients With Early-Stage HER2+ Breast Cancer Treated With Neratinib and Loperamide

Completed·PPuma Biotechnology, Inc.·Phase 2·NCT02400476·563 enrolled

Study Evaluating Neratinib (HKI-272) In Combination With Vinorelbine In Subjects With Solid Tumors And Metastatic Breast Cancer

Completed·PPuma Biotechnology, Inc.·Phase 1/2·NCT00706030·92 enrolled

Study Evaluating The Combination Of Neratinib And Capecitabine In Solid Tumors And Breast Cancer

Completed·PPuma Biotechnology, Inc.·Phase 1/2·NCT00741260·105 enrolled

A Study to Characterize Colon Pathology in Patients With HER2 Amplified Breast Cancer Treated With Neratinib

Completed·PPuma Biotechnology, Inc.·Phase 2·NCT04366713·6 enrolled

Neratinib in Extended Adjuvant Treatment for HER2+ Early Breast Cancer With pCR But High-Risk Features: A Hebei Multi-Center Real-World Study

Not yet recruiting·HHebei Medical University Fourth Hospital··NCT07019272·170 enrolled

Genetically-informed Therapy for ER+ Breast Cancer Post-CDK4/6 Inhibitor

Recruiting·—·Phase 2·NCT05933395·135 enrolled

The UK Plasma Based Molecular Profiling of Advanced Breast Cancer to Inform Therapeutic CHoices (plasmaMATCH) Trial

Unknown status·IInstitute of Cancer Research, United Kingdom·Phase 2·NCT03182634·1,150 enrolled

A Study of Neratinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in Patients With HER2+ Metastatic Breast Cancer Who Have Received Two or More Prior HER2 Directed Regimens in the Metastatic Setting

Completed·PPuma Biotechnology, Inc.·Phase 3·NCT01808573·621 enrolled

I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer

Recruiting·QQuantumLeap Healthcare Collaborative·Phase 2·NCT01042379·5,000 enrolled

Study Evaluating HKI-272 (Neratinib) In Subjects With Advanced Breast Cancer

Completed·PPuma Biotechnology, Inc.·Phase 2·NCT00300781·136 enrolled

T-DXd With or Without Neratinib for HER2 Positive Breast Cancer With Brain Metastasis

Not yet recruiting·FFudan University·Phase 2·NCT07152782·202 enrolled

Neratinib and Capmatinib Combination (Phase Ib/II) in Metastatic Breast Cancer and Inflammatory Breast Cancer Patients With Abnormal HER-family and c-Met Pathway Activity as Measured by the CELsignia Signaling Analysis Test

Terminated·MM.D. Anderson Cancer Center·Phase 1/2·NCT05243641·10 enrolled

Trial of Pre-operative Neratinib and Endocrine Therapy With Trastuzumab in ER-Positive, HER-2 Positive Breast Cancers

Recruiting·RRuth O'Regan·Phase 2·NCT04886531·30 enrolled

Neratinib Dose Escalation Regimen for HER2 Positive Early Breast Cancer

Unknown status·CChinese Academy of Medical Sciences·Phase 2·NCT05154396·60 enrolled

Fulvestrant + Neratinib In Breast Cancer

Withdrawn·MMassachusetts General Hospital·Phase 2·NCT04901299

Study Evaluating The Effects Of Neratinib After Adjuvant Trastuzumab In Women With Early Stage Breast Cancer

Completed·PPuma Biotechnology, Inc.·Phase 3·NCT00878709·2,840 enrolled

Adjuvant Therapy With Neratinib in HER2 Positive Early Breast Cancer

Recruiting·SShu Wang··NCT06693024·2,806 enrolled

Three Antidiarrheal Strategies in HER2+/HR+ Early Breast Cancer Patients Treated With Extended Adjuvant Neratinib

Active, not recruiting·SSpanish Breast Cancer Research Group·Phase 2·NCT05252988·177 enrolled

Neratinib in Treating Older Patients With Stage IV HER2-Positive Breast Cancer

Completed·—·Phase 2·NCT02673398·25 enrolled

Kadcyla And Neratinib for Interception of HER2+ Breast Cancer With Molecular Residual Disease

Recruiting·UUniversity Health Network, Toronto·Phase 2·NCT05388149·15 enrolled

Study Evaluating Neratinib Plus Paclitaxel VS Trastuzumab Plus Paclitaxel In ErbB-2 Positive Advanced Breast Cancer

Completed·PPuma Biotechnology, Inc.·Phase 2·NCT00915018·479 enrolled

Incidence and Severity of Diarrhea in Patients With HER2 Positive Breast Cancer Treated With Trastuzumab and Neratinib

Completed·UUniversity of California, San Francisco·Phase 2·NCT03094052·11 enrolled

Study Evaluating Neratinib Versus Lapatinib Plus Capecitabine For ErbB2 Positive Advanced Breast Cancer

Completed·PPuma Biotechnology, Inc.·Phase 2·NCT00777101·233 enrolled

Evaluation of Neratinib for Treatment and Prevention of Subsequent CNS Event(s) in Patients With Brain Metastasis of Advanced HER2 Positive Breast Cancer

Withdrawn·JJules Bordet Institute·Phase 2·NCT04856475

Capecitabine 7/7 Schedule With Neratinib in Patients With Metastatic HER2-Positive Breast Cancer

Active, not recruiting·MMemorial Sloan Kettering Cancer Center·Phase 1/2·NCT03377387·34 enrolled

A Dose-Escalation Study Evaluating the Combination of Trastuzumab Emtansine (T-DM1) With Neratinib in Women With Metastatic HER2-Positive Breast Cancer

Completed·NNSABP Foundation Inc·Phase 1/2·NCT02236000·49 enrolled

Neratinib +/- Fulvestrant in HER2+, ER+ Metastatic Breast Cancer

Terminated·—·Phase 2·NCT03289039·21 enrolled

Temsirolimus Plus Neratinib for Patients With Metastatic HER2-Amplified or Triple Negative Breast Cancer

Completed·PPuma Biotechnology, Inc.·Phase 1/2·NCT01111825·99 enrolled

Neratinib +/- Fulvestrant in Metastatic HER2 Non-amplified But HER2 Mutant Breast Cancer

Completed·WWashington University School of Medicine·Phase 2·NCT01670877·56 enrolled

Advanced or Metastatic Solid Tumors2 trials

Study Evaluating Neratinib In Combination With Vinorelbine In Subjects With Advanced Or Metastatic Solid Tumors

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00958724·6 enrolled

Neratinib and Everolimus, Palbociclib, or Trametinib in Treating Participants With Refractory and Advanced or Metastatic Solid Tumors With EGFR Mutation/Amplification, HER2 Mutation/Amplification, or HER3/4 Mutation or KRAS Mutation

Active, not recruiting·MM.D. Anderson Cancer Center·Phase 1·NCT03065387·93 enrolled

Advanced Solid Tumors2 trials

Neratinib Tablets Monotherapy for Advanced Solid Tumors With HER2 Mutations

Not yet recruiting·CConvalife (Shanghai) Co., Ltd.·Phase 2·NCT06519110·60 enrolled

A Study Of The Safety And Tolerability Of HKI-272 Administered Orally To Japanese Subjects With Advanced Solid Tumors

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00397046·21 enrolled

Tics2 trials

Study Evaluating The Potential Effect Of Rifampin On The Pharmacokinetics Of Neratinib

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00864487·24 enrolled

Study Evaluating The Effect Of A High-Fat Meal On The Pharmacokinetics Of Neratinib

Withdrawn·PPuma Biotechnology, Inc.·Phase 1·NCT00932464

Solid Tumors2 trials

Basket Study of Neratinib in Participants With Solid Tumors Harboring Somatic HER2 or EGFR Exon 18 Mutations

Terminated·PPuma Biotechnology, Inc.·Phase 2·NCT01953926·582 enrolled

Study Evaluating Neratinib In Combination With Temsirolimus In Subjects With Solid Tumors

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00838539·63 enrolled

27 more indications

Single Dose2 trials

A Single Dose Bioequivalence Study Of Neratinib In Healthy Subjects

Completed·PPuma Biotechnology, Inc.··NCT01142063·28 enrolled

Study Evaluating The Potential Effect Of Multiple Doses Of Neratinib On The Pharmacokinetics Of A Single Dose Of Digoxin

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00860223·27 enrolled

Metastatic Colorectal Cancer2 trials

Study of Neratinib +Trastuzumab or Neratinib + Cetuximab in Patients With KRAS/NRAS/BRAF/PIK3CA Wild-Type Metastatic Colorectal Cancer by HER2 Status

Unknown status·NNSABP Foundation Inc·Phase 2·NCT03457896·35 enrolled

Safety and Efficacy Study of Neratinib and Cetuximab to Treat Patients With Quadruple Wild-Type Metastatic Colorectal Cancer

Withdrawn·NNSABP Foundation Inc·Phase 1/2·NCT01960023

Treatment2 trials

Treatment Patterns of Neratinib in HER2+ EBC in China

Not yet recruiting·PPierre Fabre Medicament··NCT05491057·500 enrolled

Safety and Dose Finding Study of Neratinib in Children and Young Adults With Cancer That Has Returned or Not Responded to Treatment

Active, not recruiting·MMemorial Sloan Kettering Cancer Center·Phase 1/2·NCT02932280·14 enrolled

Tumors1 trial

Study Evaluating HKI-272 in Tumors

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00146172·73 enrolled

Biliary Cancer1 trial

Personalized Medicine for Advanced Biliary Cancer Patients

Recruiting·UUNICANCER·Phase 3·NCT05615818·800 enrolled

Capecitabine1 trial

A Study Of Neratinib (HKI-272) And Capecitabine In Japanese With Solid Tumor

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT01128842·7 enrolled

Cardiac Repolarization1 trial

Study to Examine the Effect of HKI-272 on Rhythms of the Heart (Cardiac Repolarization)

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00708903·60 enrolled

Esophageal Cancer1 trial

Neratinib In Combination With Chemotherapy/Trastuzumab/Pembrolizumab In HER2 Gastroesophageal Cancer

Recruiting·HH. Lee Moffitt Cancer Center and Research Institute·Phase 2·NCT06109467·36 enrolled

Patients With Advanced Solid Tumors1 trial

Phase1 of Neratinib+Trastuzumab, Pertuzumab, Paclitaxel in Patients With Advanced Solid Tumors/HER2+

Terminated·MMichelle Melisko·Phase 1·NCT02593708·6 enrolled

Advanced NSCLC1 trial

Neratinib Tablets in the Treatment of Advanced NSCLC With Rare EGFR Mutations

Unknown status·CConvalife (Shanghai) Co., Ltd.·Phase 2·NCT06029816·42 enrolled

Liver Disease1 trial

Study Evaluating The PK And Safety Of Neratinib In Healthy Subjects And Subjects With Chronic Liver Disease

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00781430·27 enrolled

Ovarian Cancer1 trial

Niraparib and Neratinib in Advanced Solid Tumors With Expansion Cohort in Advanced Ovarian Cancer

Active, not recruiting·VVirginia Commonwealth University·Phase 1·NCT04502602·18 enrolled

TNBC1 trial

Neratinib in Combination With Ruxolitinib in Patients With mTNBC

Recruiting·—·Phase 1·NCT06008275·20 enrolled

NF2-related schwannomatosis1 trial

Innovative Trial for Understanding the Impact of Targeted Therapies in NF2-Related Schwannomatosis (INTUITT-NF2)

Active, not recruiting·—·Phase 2·NCT04374305·100 enrolled

Interaction1 trial

HKI-272 Ketoconazole Drug Interaction Study

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00380328·24 enrolled

Oral1 trial

Study Evaluating Oral Administrations of HKI-272 in Healthy Male Subjects

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00550212·6 enrolled

Non-Small Cell Lung Cancer1 trial

Neratinib With and Without Temsirolimus for Patients With HER2 Activating Mutations in Non-Small Cell Lung Cancer

Completed·PPuma Biotechnology, Inc.·Phase 2·NCT01827267·62 enrolled

Glioblastoma1 trial

INdividualized Screening Trial of Innovative Glioblastoma Therapy (INSIGhT)

Recruiting·PPatrick Wen, MD·Phase 2·NCT02977780·460 enrolled

Bladder Cancer1 trial

Single Subject Neratinib in Bladder Cancer (NRR)

No longer available·UUNC Lineberger Comprehensive Cancer Center··NCT01956253

Trial1 trial

Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial

Terminated·OOHSU Knight Cancer Institute·Phase 1·NCT03878524·2 enrolled

Solid Tumor1 trial

Study Evaluating Safety And Tolerability, Solid Tumor

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00768469·10 enrolled

Prostate Cancer1 trial

Neratinib in Patients With Metastatic Castration-Resistant Prostate Cancer

Withdrawn·—·Phase 2·NCT04781374

Triple Negative1 trial

Evaluating the Efficacy of Neratinib on Live Cell HER2 Signaling Transduction Analysis Positive Triple Negative Breast

Unknown status·WWest Cancer Center·Phase 2·NCT03812393·27 enrolled

Adult Subject1 trial

Study Comparing 2 New Formulations of HKI-272 in Healthy Adult Subjects

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00498745·36 enrolled

Solid Tumor, Adult1 trial

Phase 1/2 Study of Neratinib and Divalproex Sodium (Valproate) in Advanced Solid Tumors, With an Expansion Cohort in Ras-Mutated Cancers

Suspended·VVirginia Commonwealth University·Preclinical·NCT03919292·83 enrolled

Pancreatic Ductal Carcinoma1 trial

ADOPT: Adaptive Organoid-Based Precision Therapy Study in Pancreatic Cancer - A Prospective Single-Arm Phase II Trial

Recruiting·UUniversity Health Network, Toronto·Phase 2·NCT06813079·25 enrolled

Unspecified5 trials

Open-label PK Study to Evaluate Lansoprazole and Neratinib in Healthy Subjects

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT02334501·15 enrolled

Study Evaluating HKI-272 Administered to Healthy Subjects

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00366600·56 enrolled

Study Evaluating TwoTablet Formulations of Neratinib (HKI-272)

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00814060·24 enrolled

Show 2 more trials

Study Evaluating The Tolerability Of Multiple Doses Of HKI-272

Completed·PPuma Biotechnology, Inc.·Phase 1·NCT00757809·50 enrolled

Real-life Pan-HER-blockade With Neratinib

Completed·PPierre Fabre Pharma GmbH··NCT04388384·304 enrolled

Regulatory

FDA Approval Timeline[5]

Jul 17, 2017

NERLYNX

NDA NDA208051

Sources

References

[1]
ClinicalTrials.gov — 75 trial records for neratinib. U.S. National Library of Medicine, National Institutes of Health.
[2]
MedlinePlus Drug Information — Nerlynx drug information. U.S. National Library of Medicine, National Institutes of Health.
[3]
ChEMBL — neratinib compound record. European Bioinformatics Institute (EMBL-EBI).
[4]
Open Targets Platform — Drug–disease associations for neratinib. EMBL-EBI & Wellcome Sanger Institute.
[5]
OpenFDA — FDA approval records (NDA NDA208051). U.S. Food & Drug Administration.
[6]
FDA Orange Book — Patent and exclusivity data for Nerlynx. U.S. Food & Drug Administration.
[7]
SEC EDGAR — Puma Biotechnology, Inc. company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Mechanism of Action: Epidermal Growth Factor Receptor Erbb1 Inhibitor; Receptor Protein-Tyrosine Kinase Erbb-2 Inhibitor; Receptor Protein-Tyrosine Kinase Erbb-4 Inhibitor[3]
Modality: Small molecule[3]
Highest Phase: Approved[1]
Company: PPuma Biotechnology, Inc.

Patent Landscape[6]

Patent Cliff

Oct 15, 2028

Earliest patent expiration — generic entry possible after this date

Patent #Expires

10035788Oct 15, 2028

9630946Oct 15, 2028

9139558Oct 15, 2028

9265784Aug 4, 2029

9211291Mar 24, 2030

4 more patents

8790708Nov 5, 2030

8518446Nov 20, 2030

7399865Dec 29, 2030

8669273Jul 18, 2031

Nerlynx

Status by Indication[4][1]

Competitive Landscape

Expected Milestones

Q4 2026

Q3 2027

Q1 2028

Q2 2028

Trials by Indication[1]

Breast Cancer33 trials

Advanced or Metastatic Solid Tumors2 trials

Advanced Solid Tumors2 trials

Tics2 trials

Solid Tumors2 trials

Single Dose2 trials

Metastatic Colorectal Cancer2 trials

Treatment2 trials

Tumors1 trial

Biliary Cancer1 trial

Capecitabine1 trial

Cardiac Repolarization1 trial

Esophageal Cancer1 trial

Patients With Advanced Solid Tumors1 trial

Advanced NSCLC1 trial

Liver Disease1 trial

Ovarian Cancer1 trial

TNBC1 trial

NF2-related schwannomatosis1 trial

Interaction1 trial

Oral1 trial

Non-Small Cell Lung Cancer1 trial

Glioblastoma1 trial

Bladder Cancer1 trial

Trial1 trial

Solid Tumor1 trial

Prostate Cancer1 trial

Triple Negative1 trial

Adult Subject1 trial

Solid Tumor, Adult1 trial

Pancreatic Ductal Carcinoma1 trial

Unspecified5 trials

FDA Approval Timeline[5]

References

Drug Info

Quick Facts

Patent Landscape[6]

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