Pirtobrutinib
Generic Name: pirtobrutinib
Brand Names:
Jaypirca
11 DESCRIPTION Pirtobrutinib is a kinase inhibitor. It is an orally available, small molecule ATP-competitive inhibitor of BTK. The active pharmaceutical ingredient is pirtobrutinib with the molecular formula C 22 H 21 F 4 N 5 O 3 and a molecular weight of 479.44 g/mol. The chemical name for pirtobrutinib is 5-amino-3-{4-[(5-fluoro-2-methoxybenzamido)methyl]phenyl}-1-[(2 S )-1,1,1-trifluoropropan-2-yl]-1 H -pyrazole-4-carboxamide.
Overview
11 DESCRIPTION Pirtobrutinib is a kinase inhibitor. It is an orally available, small molecule ATP-competitive inhibitor of BTK. The active pharmaceutical ingredient is pirtobrutinib with the molecular formula C 22 H 21 F 4 N 5 O 3 and a molecular weight of 479.44 g/mol. The chemical name for pirtobrutinib is 5-amino-3-{4-[(5-fluoro-2-methoxybenzamido)methyl]phenyl}-1-[(2 S )-1,1,1-trifluoropropan-2-yl]-1 H -pyrazole-4-carboxamide.
Uses
1 INDICATIONS AND USAGE JAYPIRCA ® is a kinase inhibitor indicated for the treatment of: Adult patients with relapsed or refractory mantle cell lymphoma (MCL) after at least two lines of systemic therapy, including a BTK inhibitor. ( 1.1 ). This indication is approved under accelerated approval based on response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial. Adult patients with relapsed or refractory chronic lymphocytic leukemia or small lymphocytic lymphoma (CLL/SLL) who have previously been treated with a covalent BTK inhibitor. ( 1.2 ).
Dosage
2 DOSAGE AND ADMINISTRATION Recommended dosage: 200 mg orally once daily; swallow whole with water, with or without food. Do not cut, crush, or chew tablets. ( 2.1 ) Manage toxicity using treatment interruption, dosage reduction, or discontinuation. ( 2.2 ) Reduce dose in patients with severe renal impairment. ( 2.3 , 8.6 ) 2.1 Recommended Dosage The recommended dosage of JAYPIRCA is 200 mg orally once daily until disease progression or unacceptable toxicity. Advise patients of the following: Swallow tablets whole with water. Do not cut, crush, or chew tablets. Take JAYPIRCA at the same time each day. JAYPIRCA may be taken with or without food. If a dose of JAYPIRCA is missed by more than 12 hours, do not make up the dose and take the next dose as scheduled.
Side Effects
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Infections [see Warnings and Precautions ( 5.1 )] Hemorrhage [see Warnings and Precautions ( 5.2 )] Cytopenias [see Warnings and Precautions ( 5.3 )] Atrial Fibrillation and Atrial Flutter [see Warnings and Precautions ( 5.4 )] Second Primary Malignancies [see Warnings and Precautions ( 5.5 )] Hepatotoxicity, including DILI [see Warnings and Precautions ( 5.6 )] Most common adverse reactions (≥ 30%), including laboratory abnormalities, are fatigue, neutrophil count decreased, platelet count decreased, hemoglobin decreased, leukocytes decreased, lymphocyte count decreased and calcium decreased.
Interactions
7 DRUG INTERACTIONS Strong CYP3A Inhibitors: Avoid concomitant use. If concomitant use is unavoidable, reduce the JAYPIRCA dose. ( 2.4 , 7.1 ) Strong or Moderate CYP3A Inducers: Avoid concomitant use. If concomitant use of moderate CYP3A inducers is unavoidable, increase the JAYPIRCA dose. ( 2.5 , 7.1 ) Sensitive CYP2C8, CYP2C19, CYP3A, P-gp, or BCRP Substrates: For substrates where minimal concentration changes may increase the risk of adverse reactions, follow recommendations for co-administration with CYP2C8, CYP2C19, CYP3A, P-gp, or BCRP inhibitors provided in their approved product labeling. ( 7.2 ) 7.1 Effect of Other Drugs on JAYPIRCA Strong CYP3A Inhibitors Pirtobrutinib is a CYP3A substrate.
Warnings
5 WARNINGS AND PRECAUTIONS Infections: Monitor for signs and symptoms of infection, evaluate promptly, and treat. ( 5.1 ) Hemorrhage: Monitor for bleeding and manage appropriately. ( 5.2 ) Cytopenias: Monitor complete blood counts during treatment. ( 5.3 ) Cardiac Arrythmias: Monitor for symptoms of arrhythmias and manage appropriately. ( 5.4 ) Second Primary Malignancies: Other malignancies have developed, including skin cancers and other carcinomas. Monitor and advise patients to use sun protection. ( 5.5 ) Hepatotoxicity, Including Drug-Induced Liver Injury: Monitor hepatic function throughout treatment. ( 5.6 ) Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of potential risk to a fetus and to use effective contraception. 4 CONTRAINDICATIONS None. None ( 4 ).
Pregnancy
8.1 Pregnancy Risk Summary Based on findings from animal studies, JAYPIRCA can cause fetal harm when administered to a pregnant woman. There are no available data on JAYPIRCA use in pregnant women to evaluate for a drug-associated risk. In an animal reproduction study, administration of pirtobrutinib to pregnant rats during organogenesis resulted in adverse developmental outcomes, including structural abnormalities, altered fetal growth, and embryo-fetal mortality, at maternal exposures approximately 3-times those in patients at the recommended daily dose of 200 mg (see Data).
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied JAYPIRCA tablets are supplied as follows: Tablet Strength Description Package Configuration NDC Number 50 mg Blue, film coated, arc-triangle shaped tablets debossed with “Lilly 50” on one side and “6902” on the other side. Bottle with child-resistant closure. Each bottle contains 30 tablets.
Frequently Asked Questions
What is Pirtobrutinib used for?▼
1 INDICATIONS AND USAGE JAYPIRCA ® is a kinase inhibitor indicated for the treatment of: Adult patients with relapsed or refractory mantle cell lymphoma (MCL) after at least two lines of systemic therapy, including a BTK inhibitor. ( 1.1 ). This indication is approved under accelerated approval based on response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial. Adult patients with relapsed or refractory chronic lymphocytic leukemia or small lymphocytic lymphoma (CLL/SLL) who have previously been treated with a covalent BTK inhibitor. ( 1.2 ).
What are the side effects of Pirtobrutinib?▼
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Infections [see Warnings and Precautions ( 5.1 )] Hemorrhage [see Warnings and Precautions ( 5.2 )] Cytopenias [see Warnings and Precautions ( 5.3 )] Atrial Fibrillation and Atrial Flutter [see Warnings and Precautions ( 5.4 )] Second Primary Malignancies [see Warnings and Precautions ( 5.5 )] Hepatotoxicity, including DILI [see Warnings and Precautions ( 5.6 )] Most common adverse reactions (≥ 30%), including laboratory abnormalities, are fatigue, neutrophil count decreased, platelet count decreased, hemoglobin decreased, leukocytes decreased, lymphocyte count decreased and calcium decreased.
Can I take Pirtobrutinib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on findings from animal studies, JAYPIRCA can cause fetal harm when administered to a pregnant woman. There are no available data on JAYPIRCA use in pregnant women to evaluate for a drug-associated risk. In an animal reproduction study, administration of pirtobrutinib to pregnant rats during organogenesis resulted in adverse developmental outcomes, including structural abnormalities, altered fetal growth, and embryo-fetal mortality, at maternal exposures approximately 3-times those in patients at the recommended daily dose of 200 mg (see Data).
What are the important warnings for Pirtobrutinib?▼
5 WARNINGS AND PRECAUTIONS Infections: Monitor for signs and symptoms of infection, evaluate promptly, and treat. ( 5.1 ) Hemorrhage: Monitor for bleeding and manage appropriately. ( 5.2 ) Cytopenias: Monitor complete blood counts during treatment. ( 5.3 ) Cardiac Arrythmias: Monitor for symptoms of arrhythmias and manage appropriately. ( 5.4 ) Second Primary Malignancies: Other malignancies have developed, including skin cancers and other carcinomas. Monitor and advise patients to use sun protection. ( 5.5 ) Hepatotoxicity, Including Drug-Induced Liver Injury: Monitor hepatic function throughout treatment. ( 5.6 ) Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of potential risk to a fetus and to use effective contraception. 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.