Lorlatinib

Lorlatinib produced by Lucius Pharmaceuticals is available in two sizes, 25mg and 100mg, to meet the treatment needs of different patients.

As a professional pharmaceutical company, Lucius Pharmaceuticals focuses on the quality assurance of drugs. The Lorlatinib produced by it has undergone strict quality inspection and certification.

Lorlatinib is an anticancer drug used to treat non-small cell lung cancer. The drug specifically targets ALK and ROS1-driven non-small cell lung cancer, providing patients with a new treatment option.

1.Main ingredient

Lorlatinib

2.Applicable people

Adult patients with metastatic non-small cell carcinoma.

3.Use in Specific Populations

3.1 Pregnancy  

Based on findings from animal studies and its mechanism of action,  Lorlatinib can cause embryo-fetal harm when administered to a pregnant woman. There are no available  data on Lorlatinib use in pregnant women. Administration of lorlatinib to pregnant rats and rabbits by oral  gavage during the period of organogenesis resulted in malformations, increased post-implantation loss, and  abortion at maternal exposures that were equal to or less than the human exposure at the recommended dose of  100 mg once daily based on AUC (see Data). Advise a pregnant woman of the potential risk to a fetus.  

3.2 Lactation  

There are no data on the presence of lorlatinib or its metabolites in either human or animal milk or its effects on  the breastfed infant or on milk production. Because of the potential for serious adverse reactions in breastfed  infants, instruct women not to breastfeed during treatment with Lorlatinib and for 7 days after the final dose.

3.3 Females and Males of Reproductive Potential  

Females  

Advise female patients of reproductive potential to use effective non-hormonal contraception during treatment  with Lorlatinib and for at least 6 months after the final dose. Advise females of reproductive potential to use  a non-hormonal method of contraception, because Lorlatinib can render hormonal contraceptives ineffective.  

Males  

Based on genotoxicity findings, advise males with female partners of reproductive potential to use effective  contraception during treatment with Lorlatinib and for at least 3 months after the final dose.  

3.4 Pediatric Use  

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

3.5 Geriatric Use  

Of the patients in Study B7461001 (N=295) and Study B7461006 (N=149) who received 100 mg Lorlatinib  orally once daily, 18% and 40% of patients, respectively, were aged 65 years or older. No clinically important differences in safety or efficacy were observed between patients aged 65 years or older and younger patients.

3.6 Hepatic Impairment  

No dose adjustment is recommended for patients with mild hepatic impairment (total bilirubin ≤ upper limit of  normal [ULN] with AST > ULN or total bilirubin >1 to 1.5 × ULN with any AST). The recommended dose of  Lorlatinib has not been established for patients with moderate (total bilirubin ≥ 1.5 to 3.0 × ULN with any  AST) or severe (total bilirubin > 3.0 × ULN with any AST) hepatic impairment.

3.7 Renal Impairment  

Reduce the dose when administering Lorlatinib to patients with severe (CLcr 15 to <30 mL/min, estimated  by Cockcroft Gault) renal impairment.

No dose adjustment is recommended for patients with mild or moderate renal impairment (creatinine clearance  [CLcr] 30 to 89 mL/min estimated by Cockcroft-Gault).

4.Storage

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).

5.Pharmacokinetics

The median lorlatinib Tmax was 1.2 hours (0.5 to 4 hours) following a single oral 100 mg dose and 2 hours  (0.5 to 23 hours) following 100 mg orally once daily at steady-state.  

The mean absolute bioavailability is 81% (90% CI 75.7%, 86.2%) after oral administration compared to  intravenous administration.  

FDA,2021.03