Osimertinib

Osimertinib is an oral, irreversible, third-generation EGFR inhibitor developed by AstraZeneca Pharmaceuticals in the UK. Lucius produces Osimertinib with a drug specification of 80mg.

Osimertinib first received accelerated approval from the US Food and Drug Administration (FDA) in November 2015 for the treatment of advanced non-small cell lung cancer with EGFR T790M mutation.

EGFR is a receptor that exists on the surface of cells, and mutations in it can cause abnormal cell proliferation, leading to the development of lung cancer. Osimertinib inhibits tumor cell proliferation and growth by suppressing EGFR mutations, preventing their activation.

1.Main components

Osimertinib

2.Adapt to the population

Patients with advanced renal cell carcinoma, differentiated thyroid carcinoma, advanced non-small cell lung cancer, liver cancer, and advanced prostate cancer.

3.Medication for special populations

3.1Pregnancy

Osimertinib can cause fetal harm when administered to a pregnant woman. There are no available data on Osimertinib use in pregnant women. Advise pregnant women of the potential risk to a fetus.

3.2Lactation

There are no data on the presence of Osimertinib or its active metabolites in human milk, the effects of Osimertinib on the breastfed infant or on milk production.advise women not to breastfeed during treatment with Osimertinib and for 2 weeks after the final dose.

3.3Females and Males of Reproductive Potential

Advise females of reproductive potential to use effective contraception during treatment with Osimertinib and for 6 weeks after the final dose.

Advise male patients with female partners of reproductive potential to use effective contraception during and for 4 months following the final dose of Osimertinib. 

3.4Pediatric Use

The safety and effectiveness of Osimertinib in pediatric patients have not been established.

3.5Geriatric Use

No overall differences in effectiveness were observed based on age. Exploratory analysis suggests a higher incidence of Grade 3 and 4 adverse reactions (35% vs 27%) and more frequent dose modifications for adverse reactions (32% vs 21%) in patients 65 years or older as compared to those younger than 65 years.

3.6Hepatic Impairment

No dose adjustment is recommended in patients with mild to moderate hepatic impairment . There is no recommended dose for Osimertinib for patients with severe hepatic impairment. 

3.7Renal Impairment

No dose adjustment is recommended in patients with creatinine clearance(CLcr) 15 - 89 mL/min.There is no recommended dose of Osimertinib for patients with end-stage renal disease.

4.Drug overdose

Drug overdose is not yet clear.

5.Drug storage

Store Osimertinib bottles at 25°C (77°F). Excursions permitted to 15-30°C (59-86°F).

6.Pharmacokinetics

The median time to Cmax of osimertinib was 6 hours (range 3-24 hours).

from FDA，2022.10