Sevabertinib
Generic Name: sevabertinib
Brand Names:
Hyrnuo
11 DESCRIPTION HYRNUO tablets contain sevabertinib, a kinase inhibitor. The chemical name of the drug substance is 3-(3-chloro-2-methoxyanilino)-2-{3-[(2S)-1,4-dioxan-2-ylmethoxy]pyridin-4-yl}-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one hydrate. The molecular formula is C 24 H 25 ClN 4 O 5 (anhydrate) and the molecular weight is 484.93 g/mol (anhydrate).
Overview
11 DESCRIPTION HYRNUO tablets contain sevabertinib, a kinase inhibitor. The chemical name of the drug substance is 3-(3-chloro-2-methoxyanilino)-2-{3-[(2S)-1,4-dioxan-2-ylmethoxy]pyridin-4-yl}-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one hydrate. The molecular formula is C 24 H 25 ClN 4 O 5 (anhydrate) and the molecular weight is 484.93 g/mol (anhydrate).
Uses
1 INDICATIONS AND USAGE 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) ] . Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.
Dosage
2 DOSAGE AND ADMINISTRATION 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) ] .
Side Effects
6 ADVERSE REACTIONS 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.
Interactions
7 DRUG INTERACTIONS Strong CYP3A Inhibitors: Avoid concomitant use with strong CYP3A inhibitors. If concomitant use cannot be avoided, reduce HYRNUO dosage. ( 2.4 , 7.1 ). Moderate CYP3A Inhibitors: Monitor patients for increased HYRNUO-associated adverse reactions ( 2.3 , 7.1 ) Strong and Moderate CYP3A Inducers: Avoid concomitant use with strong or moderate CYP3A inducers. ( 7.1 ) Certain CYP3A Substrates: Avoid concomitant use with CYP3A substrates where minimal increases in concentration may lead to serious adverse reactions unless otherwise recommended in the Prescribing Information of the CYP3A substrate.
Warnings
5 WARNINGS AND PRECAUTIONS 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. 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
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.
Storage
Storage and Handling Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [ see USP Controlled Room Temperature ].
Frequently Asked Questions
What is Sevabertinib used for?▼
1 INDICATIONS AND USAGE 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) ] . Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.
What are the side effects of Sevabertinib?▼
6 ADVERSE REACTIONS 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.
Can I take Sevabertinib during pregnancy?▼
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.
What are the important warnings for Sevabertinib?▼
5 WARNINGS AND PRECAUTIONS 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. 4 CONTRAINDICATIONS None. None. ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.