Exkivity

Exkivity was originally developed and produced by Takeda Corporation in Japan as an oral small molecule tyrosine kinase inhibitor, with a drug specification of 40mg * 120pills。

On September 16, 2021, the FDA officially approved the launch of Exkivity, becoming the second globally approved targeted therapy for EGFR exon 20 insertion mutation lung cancer patients.

Exkivity inhibits the phosphorylation of EGFR, particularly targeting the insertion mutation of EGFR exon 20, blocking the signaling pathway of tumor cells and inhibiting their growth and proliferation. 

1.Main components

Exkivity

2.Adapt to the population

Adult patients with locally advanced or metastatic non-small cell lung cancer.

3.Medication for special populations

3.1Pregnant

There are no available data on Exkivity use in pregnant women. Oral administration of mobocertinib to pregnant rats during the period of organogenesis resulted in embryolethality (embryo-fetal death) and maternal toxicity at plasma exposures approximately 1.7 times the human exposure based on AUC at the 160 mg once daily clinical dose (see Data). Advise pregnant women of the potential risk to a fetus.

3.2Lactation 

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

3.3Females and Males of Reproductive Potential 

Advise females of reproductive potential to use effective non-hormonal contraception during  treatment with Exkivity and for 1 month after the last dose. Exkivity may render hormonal  contraceptives ineffective .Advise males with female partners of reproductive potential to use effective contraception during  treatment with Exkivity and for 1 week after the last dose.

3.4Geriatric Use

No overall difference in effectiveness was observed between patients aged 65 and older and younger patients. Exploratory analysis suggests a higher incidence of Grade 3 and 4 adverse reactions (69% vs 47%) and serious adverse reactions (64% vs 35%) in patients 65 years and older as compared to those younger than 65 years.

3.5Pediatric Use

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

3.6Renal Impairment

Mobocertinib plasma concentrations are higher in patients with severe renal impairment which may increase the risk of adverse reactions. Reduce the recommended dosage of Exkivity for patients with severe renal impairment .No dosage adjustment of Exkivity is recommended for patients with mild-to-moderate renal impairment .

3.7Hepatic Impairment

No dosage adjustment of Exkivity is recommended for patients with mild -to-severehepatic impairment .

4.Drug overdose

Drug overdose is not yet clear.

5.Drug storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted from 15°C to 30°C (59°F to 86°F).

6.Pharmacokinetics

The median (min, max) time to peak concentration (Tmax) of mobocertinib is 4 hours (1, 8 hours). The mean (%CV) absolute bioavailability is 37% (50%).

from FDA，2023.09