Osimertinib
Generic Name: osimertinib
Brand Names:
Tagrisso
11 DESCRIPTION Osimertinib is a kinase inhibitor for oral use. The molecular formula for osimertinib mesylate is C 28 H 33 N 7 O 2 •CH 4 O 3 S, and the molecular weight is 596 g/mol. The chemical name is N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide mesylate salt.
Overview
11 DESCRIPTION Osimertinib is a kinase inhibitor for oral use. The molecular formula for osimertinib mesylate is C 28 H 33 N 7 O 2 •CH 4 O 3 S, and the molecular weight is 596 g/mol. The chemical name is N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide mesylate salt.
Uses
1 INDICATIONS AND USAGE TAGRISSO is a kinase inhibitor indicated for: • adjuvant therapy after tumor resection in adult patients with non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. ( 1.1 , 2.2 ) • the treatment of adult patients with locally advanced, unresectable (stage III) NSCLC whose disease has not progressed during or following concurrent or sequential platinum-based chemoradiation therapy and whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.
Dosage
2 DOSAGE AND ADMINISTRATION Adjuvant treatment of early-stage NSCLC: 80 mg orally once daily, with or without food, until disease recurrence, or unacceptable toxicity, or for up to 3 years. ( 2.3 ) Locally advanced, unresectable (stage III) NSCLC: Following platinum-based chemoradiation therapy, 80 mg orally once daily, with or without food, until disease progression or unacceptable toxicity. ( 2.3 ) Metastatic NSCLC: 80 mg orally once daily, with or without food, until disease progression or unacceptable toxicity. ( 2.3 ) Locally advanced or metastatic NSCLC: 80 mg orally once daily administered in combination with pemetrexed and platinum-based chemotherapy, with or without food, until disease progression or unacceptable toxicity due to TAGRISSO.
Side Effects
6 ADVERSE REACTIONS The following adverse reactions are discussed in greater detail in other sections of the labeling: • Interstitial Lung Disease/Pneumonitis [see Error! Hyperlink reference not valid. ] • QTc Interval Prolongation [see Error! Hyperlink reference not valid. ] • Cardiomyopathy [see Error! Hyperlink reference not valid. ] • Keratitis [see Error! Hyperlink reference not valid. ] • Erythema multiforme, Stevens-Johnson syndrome, and Toxic epidermal necrolysis [see Error! Hyperlink reference not valid. ] • Cutaneous Vasculitis [see Error! Hyperlink reference not valid. ] • Aplastic Anemia [see Error! Hyperlink reference not valid.
Interactions
7 DRUG INTERACTIONS Strong CYP3A Inducers : Avoid concomitant use. If not possible, increase TAGRISSO to 160 mg daily in patients receiving a strong CYP3A4 inducer. ( 2.5 , 7.1 ) 7.1 Effect of Other Drugs on Osimertinib Strong CYP3A Inducers Co-administering TAGRISSO with a strong CYP3A4 inducer decreased the exposure of osimertinib compared to administering TAGRISSO alone [see Clinical Pharmacology (12.3) ] . Decreased osimertinib exposure may lead to reduced efficacy. Avoid co-administering TAGRISSO with strong CYP3A inducers. Increase the TAGRISSO dosage when co-administering with a strong CYP3A4 inducer if concurrent use is unavoidable [see Dosage and Administration (2.5) ] . No dose adjustments are required when TAGRISSO is used with moderate and/or weak CYP3A inducers.
Warnings
5 WARNINGS AND PRECAUTIONS • Interstitial Lung Disease (ILD)/Pneumonitis: Monitor for new or worsening pulmonary symptoms indicative of ILD/pneumonitis. For patients receiving TAGRISSO who have not received recent definite platinum-based chemoradiation therapy, permanently discontinue TAGRISSO in patients diagnosed with ILD/Pneumonitis. For patients who received recent definitive platinum-based chemoradiation therapy with Grade 1 ILD/pneumonitis continue TAGRISSO or interrupt and restart, as appropriate. Permanently discontinue TAGRISSO in patients diagnosed with Grade ≥2 ILD/pneumonitis. ( 2.5 , Error! Hyperlink reference not valid. 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary Based on data from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , TAGRISSO can cause fetal harm when administered to a pregnant woman. There are no available data on TAGRISSO use in pregnant women. Administration of osimertinib to pregnant rats was associated with embryolethality and reduced fetal growth at plasma exposures 1.5 times the exposure at the recommended clinical dose (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING 80 mg tablets: beige, oval and biconvex tablet marked with “AZ 80” on one side and plain on the reverse and are available in bottles of 30 (NDC 0310-1350-30). 40 mg tablets: beige, round and biconvex tablet marked with “AZ 40” on one side and plain on the reverse and are available in bottles of 30 (NDC 0310-1349-30). Store TAGRISSO bottles at 25°C (77°F).
Frequently Asked Questions
What is Osimertinib used for?▼
1 INDICATIONS AND USAGE TAGRISSO is a kinase inhibitor indicated for: • adjuvant therapy after tumor resection in adult patients with non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. ( 1.1 , 2.2 ) • the treatment of adult patients with locally advanced, unresectable (stage III) NSCLC whose disease has not progressed during or following concurrent or sequential platinum-based chemoradiation therapy and whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.
What are the side effects of Osimertinib?▼
6 ADVERSE REACTIONS The following adverse reactions are discussed in greater detail in other sections of the labeling: • Interstitial Lung Disease/Pneumonitis [see Error! Hyperlink reference not valid. ] • QTc Interval Prolongation [see Error! Hyperlink reference not valid. ] • Cardiomyopathy [see Error! Hyperlink reference not valid. ] • Keratitis [see Error! Hyperlink reference not valid. ] • Erythema multiforme, Stevens-Johnson syndrome, and Toxic epidermal necrolysis [see Error! Hyperlink reference not valid. ] • Cutaneous Vasculitis [see Error! Hyperlink reference not valid. ] • Aplastic Anemia [see Error! Hyperlink reference not valid.
Can I take Osimertinib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on data from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , TAGRISSO can cause fetal harm when administered to a pregnant woman. There are no available data on TAGRISSO use in pregnant women. Administration of osimertinib to pregnant rats was associated with embryolethality and reduced fetal growth at plasma exposures 1.5 times the exposure at the recommended clinical dose (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S.
What are the important warnings for Osimertinib?▼
5 WARNINGS AND PRECAUTIONS • Interstitial Lung Disease (ILD)/Pneumonitis: Monitor for new or worsening pulmonary symptoms indicative of ILD/pneumonitis. For patients receiving TAGRISSO who have not received recent definite platinum-based chemoradiation therapy, permanently discontinue TAGRISSO in patients diagnosed with ILD/Pneumonitis. For patients who received recent definitive platinum-based chemoradiation therapy with Grade 1 ILD/pneumonitis continue TAGRISSO or interrupt and restart, as appropriate. Permanently discontinue TAGRISSO in patients diagnosed with Grade ≥2 ILD/pneumonitis. ( 2.5 , Error! Hyperlink reference not valid. 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.