Sevabertinib

Sevabertinib is a reversible kinase inhibitor of human epidermal growth factor receptor 2 (HER2). It also exhibits activity against epidermal growth factor receptor (EGFR).

• HYRNUO is indicated for the treatment of adult patients with locally advanced or metastatic non-squamous non-small cell lung cancer (NSCLC) whose tumors have HER2 ( ERBB2 ) tyrosine kinase domain (TKD) activating mutations, as detected by an FDA-approved test [see Dosage and Administration (2.1) ] , and who have received a prior systemic therapy. This indication is approved under accelerated approval based on objective response rate (ORR) and duration of response (DOR) [see Clinical Studies (14) ] .ICD-10: C34.90

• None. None.contraindicated

Select patients for treatment with HYRNUO based on the presence of HER2 ( ERBB2 ) TKD activating mutations. ( 2.1 ) Recommended Dosage : 20 mg orally twice daily with food until disease progression or unacceptable toxicity. Swallow tablets whole. ( 2.2 ) 2.1 Patient Selection Select patients for treatment of locally advanced or metastatic non-squamous NSCLC based on the presence of HER2 ( ERBB2 ) TKD activating mutations in tumor specimens [see Clinical Studies (14) ] . Information on FDA-approved tests is available at http://www.fda.gov/CompanionDiagnostics. 2.2 Recommended Dosage The recommended dosage of HYRNUO is 20 mg orally twice daily with food, until disease progression or unacceptable toxicity [see Clinical Pharmacology (12.3) ] . Swallow tablets whole. Do not cut, crush, or chew tablets. Missed Dose If a dose is missed, take the missed dose as soon as you remember prior to the next scheduled dose. Do not take 2 doses at the same time to make up for the missed dose. Vomited Dose If a dose is vomited, do not take an additional dose. Resume dosing at the next scheduled time. 2.3 Dosage Modifications for Adverse Reactions The recommended dosage reductions for adverse reactions are provided in Table 1. Table 1: Recommended HYRNUO Dosage Reductions for Adverse Reactions Dose Reduction Dosage Modification First 10 mg twice daily Second 10 mg once daily Permanently discontinue HYRNUO in patients who are unable to tolerate 10 mg once daily. The recommended dosage modifications for adverse reactions are provided in Table 2.

Diarrhea : At the first sign of diarrhea or increased bowel movement frequency, instruct patients to start an antidiarrheal treatment, and to increase their fluid and electrolyte intake. Interrupt, reduce the dose, or permanently discontinue HYRNUO based on severity. ( 5.1 ) Hepatotoxicity : Monitor liver function tests including ALT, AST, and total bilirubin at baseline prior to administration of HYRNUO, every 2 weeks during the first month, and then monthly thereafter as clinically indicated, with more frequent testing in patients who develop transaminase elevations. Interrupt, reduce the dose, or permanently discontinue HYRNUO based on severity. ( 5.2 ) Interstitial Lung Disease (ILD)/Pneumonitis : Monitor patients for new or worsening symptoms indicative of ILD/pneumonitis (e.g., dyspnea, cough, fever). Discontinue HYRNUO upon confirmation of ILD/pneumonitis. ( 5.3 ) Ocular Toxicity : Promptly refer patients presenting with new or worsening eye symptoms to an ophthalmologist. Interrupt, reduce the dose or permanently discontinue HYRNUO based on severity. ( 5.4 ) Pancreatic Enzyme Elevation : Monitor amylase and lipase regularly during treatment. Interrupt, reduce the dose, or permanently discontinue HYRNUO based on severity. ( 5.5 ) Embryo-fetal toxicity : Can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception. ( 5.6 , 8.1 , 8.3 ) 5.1 Diarrhea HYRNUO can cause severe diarrhea that can lead to dehydration and electrolyte imbalances.

The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling: Diarrhea [see Warnings and Precautions (5.1) ] Hepatotoxicity [see Warnings and Precautions (5.2) ] Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.3) ] Ocular Toxicity [see Warnings and Precautions (5.4) ] Pancreatic Enzyme Elevation [see Warnings and Precautions (5.5) ] Most common adverse reactions (>20%) : diarrhea, rash, paronychia, stomatitis, and nausea. Most common Grade 3 or 4 laboratory abnormalities (≥2%) : decreased potassium, increased lipase, decreased lymphocyte count, decreased sodium, increased amylase, increased ALT, and increased AST. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bayer HealthCare Pharmaceuticals Inc. at 1-888-842-2937 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The pooled safety population in the WARNINGS AND PRECAUTIONS reflects exposure to HYRNUO at 20 mg orally twice daily in 268 patients with locally advanced or metastatic NSCLC harboring HER2 and/or other mutations from the SOHO-01 study [see Clinical Studies (14) ] . Among 268 patients who received HYRNUO, 35% were exposed for greater than 6 months and 12% were exposed for greater than 1 year.

Lactation : Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , HYRNUO can cause fetal harm when administered to a pregnant woman. There are no available data on the use of HYRNUO in pregnant women to inform a drug-associated risk. In embryo-fetal development studies, oral administration of sevabertinib to pregnant rats during the period of organogenesis resulted in alterations to growth at maternal exposures ≥0.18 times the human exposure based on area under the curve (AUC) at the clinical dose of 20 mg twice daily. Animal studies with disrupted or depleted HER2/EGFR and in vitro assays have demonstrated that inhibition of HER2 and/or EGFR results in structural abnormalities, alteration to growth, and embryo-fetal and infant mortality (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In embryo-fetal development studies, sevabertinib was administered orally to pregnant rats during the period of organogenesis from gestation day 6 to 17 at doses ranging from 1.5 to 11 mg/kg/day.

Metabolism

Sevabertinib pharmacokinetics were observed at steady state in patients with advanced NSCLC harboring activating HER2 or EGFR mutations at the approved recommended dosage and are presented as mean (CV%), unless otherwise specified. Sevabertinib maximum concentration (C max ) is 902 (45%) ng/mL and total systemic exposure (AUC) is 6,640 (50%) ng*h/mL.

• Nov 19, 2025NDANDA219972Bayer Healthcare

1. 1Diarrhoea480%
2. 2Acute Kidney Injury120%
3. 3Defaecation Urgency120%
4. 4Erythema120%
5. 5Gastrointestinal Toxicity120%
6. 6Oedema120%
7. 7Product Use In Unapproved Indication120%

The 4 most recently updated of 4 ClinicalTrials.gov registrations naming Sevabertinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Learn More About How Well Treatment With Sevabertinib (BAY 2927088) Tablets Works and How Safe it is in Participants Who Have a Solid Tumor With Mutations of the Human Epidermal Growth Factor Receptor 2 (HER2)
  Recruiting · Phase 2 · Interventional · 111 enrolled · Bayer
  NCT06760819updated 2026-06-04
• Expanded Access to Provide Sevabertinib (BAY 2927088) for the Treatment of Locally Advanced or Metastatic NSCLC With HER2 Mutation
  Available · Expanded access · Bayer
  NCT06761976updated 2026-06-04
• A Study to Learn More About How Well Sevabertinib Works and How Safe it is Compared With Standard Treatment, in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations of the Human Epidermal Growth Factor Receptor 2 (HER2)
  Recruiting · Phase 3 · Interventional · 444 enrolled · Bayer
  NCT06452277updated 2026-05-18
• A Study Evaluating How Moderate Liver Impairment Affects the Absorption, Distribution, Metabolism, and Elimination of Sevabertinib After a Single Oral Dose
  Completed · Phase 1 · Interventional · 18 enrolled · Bayer
  NCT07102095updated 2026-02-10

Frequently asked questions

How does Sevabertinib work?

Sevabertinib is a reversible kinase inhibitor of human epidermal growth factor receptor 2 (HER2). It also exhibits activity against epidermal growth factor receptor (EGFR).

What is Sevabertinib used for?

According to FDA labeling, Sevabertinib carries indications including: HYRNUO is indicated for the treatment of adult patients with locally advanced or metastatic non-squamous non-small cell lung cancer (NSCLC) whose tumors have HER2 ( ERBB2 ) tyrosine kinase domain (TKD) activating mutations, as detected by an FDA-approved test [see Dosage and Administration (2.1) ] , and who have received a prior systemic therapy. This indication is approved under accelerated approval based on objective response rate (ORR) and duration of response (DOR) [see Clinical Studies (14) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Sevabertinib?

Sevabertinib is classified as Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Sevabertinib?

Sevabertinib is marketed under brand names including Hyrnuo.

What are the contraindications for Sevabertinib?

Sevabertinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.