Futibatinib(Lytgobi)

Futibatinib, branded as Lytgobi, is an anti-cancer drug used to treat cholangiocarcinoma by inhibiting FGFR signaling, thereby inhibiting the growth and spread of tumor cells.

The drug has shown good efficacy and safety in clinical trials, providing a new treatment option for cholangiocarcinoma patients.

Forbatinib is an effective treatment for specific types of cholangiocarcinoma. However, it is necessary to pay close attention to its side effects and safety issues during use, and use it rationally under the guidance of a doctor.

1. Main ingredient

 Futibatinib

2. Applicable people

 Select patients for the treatment of unresectable, locally advanced or metastatic intrahepatic  cholangiocarcinoma with Futibatinib based on the presence of an FGFR2 gene fusion or rearrangement. An FDA-approved test for detection of FGFR2 gene fusions or other rearrangements in  patients with unresectable, locally advanced, or metastatic intrahepatic cholangiocarcinoma for selecting  patients for treatment with Futibatinib is not available.

3. Use in Specific Populations

3.1 Pregnancy 

Based on findings in an animal study and its mechanism of action, Futibatinib can cause fetal harm or loss of  pregnancy when administered to a pregnant woman. There are no available  data on the use of Futibatinib in pregnant women. Oral administration of futibatinib to pregnant rats during the period of organogenesis at maternal plasma exposures below the human exposure at the clinical dose of 20 mg  resulted in fetal malformations, fetal growth retardation, and embryo-fetal death . Advise pregnant  women of the potential risk to a fetus.

In the U.S. general population, the estimated background risk of major birth defects and miscarriage in  clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

3.2 Lactation  

There are no data on the presence of futibatinib or its metabolites in human milk or their effects on either the  breastfed child or on milk production. Because of the potential for serious adverse reactions from Futibatinib in  breastfed children, advise women not to breastfeed during treatment and for 1 week after the last dose.

3.3 Females and Males of Reproductive Potential  

Futibatinib can cause fetal harm when administered to a pregnant woman.

3.4 Pediatric Use  

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

3.5 Geriatric Use  

Of the 103 patients treated with Futibatinib in Study TAS-120-101, 22% were 65 years or older. Based on  available data, no overall differences in safety or effectiveness of Futibatinib have been observed between  patients 65 years of age and older and younger adult patients.

4. Storage

 Store Futibatinib tablets at room temperature 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C  and 30°C (59°F to 86°F).

5. Pharmacokinetics

The pharmacokinetics of futibatinib administered 20 mg once daily were evaluated in patients with advanced  solid tumors unless otherwise specified.

Futibatinib exposure (AUC) increased proportionally over the dose range from 4 to 24 mg orally once daily (0.2  to 1.2 times the maximum approved recommended dosage). At the recommended dosage, the geometric mean  (coefficient of variation [CV] %) maximal concentration of futibatinib at steady state (Cmax,ss) was 144 ng/mL  (50%) and AUC at steady state (AUCss) was 790 ng∙hr/mL (45%), with no accumulation after repeat doses.

FDA，2022.09