Moboxen Mobocertinib capsules

[Core Drug Information]

Generic Name: Mobocertinib / Mobocertinib Succinate Capsules

Brand Name: Exkivity / Moboxen

English Name: Mobocertinib (TAK-788, AP-32788)

Formulation: Hard Capsules

Specification: 40 mg/capsule; 60 capsules/box

Manufacturer: Everest Pharma Ltd (Bangladesh)

[Indications and Mechanism of Action]

Mechanism of Action: An irreversible tyrosine kinase inhibitor specifically designed to selectively target EGFR exon 20 insertion mutations, exhibiting weak inhibitory activity against wild-type EGFR.

Indications: Indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations, whose disease has progressed on or after platinum-based chemotherapy.

Prior to use, the presence of EGFR exon 20 insertion mutations must be confirmed using a validated testing method.

[Dosage and Administration]

Recommended Dosage: 160 mg (four 40 mg capsules) orally once daily.

Administration Method: May be taken with or without food. Capsules should be swallowed whole; do not open, chew, or dissolve the capsules.

Missed Dose/Vomiting: If a dose is missed by more than 6 hours, or if vomiting occurs after administration, do not take a missed dose; resume dosing as scheduled at the usual time the following day.

Dosage Adjustment: Based on the severity of adverse reactions. The table below outlines the primary dosage adjustment schedule:

Adjustment Step: Dosage Regimen

Starting Dose: 160 mg once daily

First Dose Reduction: 120 mg once daily

Second Dose Reduction: 80 mg once daily

[Important Warnings and Precautions (Dosage Adjustment Guidelines)]

Mobocertinib carries a Boxed Warning; particular attention should be paid to the following risks:

Adverse Reaction/Condition: Management and Dosage Adjustment Recommendations

QTc Interval Prolongation and Torsades de Pointes: Monitor ECGs and electrolytes periodically at baseline and during treatment. Depending on the degree of QTc interval prolongation, measures such as temporary interruption, dose reduction, or permanent discontinuation of the drug should be implemented.

Interstitial Lung Disease (ILD)/Pneumonitis: Patients should seek immediate medical attention upon the onset of new or worsening pulmonary symptoms (e.g., dyspnea, cough, fever). If ILD is suspected, the drug should be temporarily interrupted; if ILD is confirmed, the drug must be permanently discontinued.

Heart Failure: Cardiac function (e.g., left ventricular ejection fraction) should be monitored during treatment. In the event of symptomatic heart failure or severe decline in cardiac function, the drug must be permanently discontinued.

Severe Diarrhea: The incidence is very high (approximately 93%) and may lead to dehydration and renal impairment. Anti-diarrheal treatment (e.g., loperamide) should be initiated immediately upon the first occurrence of diarrhea. Depending on the severity, temporary interruption, dose reduction, or permanent discontinuation of the drug may be required.

[Adverse Reactions]

In clinical studies, the most common adverse reactions (incidence ≥20%) included: diarrhea, rash, nausea, stomatitis, vomiting, decreased appetite, paronychia, fatigue, dry skin, and musculoskeletal pain.

The most common Grade 3–4 laboratory abnormalities (incidence ≥2%) included: increased amylase, increased lipase, lymphopenia, hypokalemia, hypomagnesemia, increased creatinine, and anemia.

[Drug Interactions]

1.  Strong CYP3A Inhibitors (e.g., ketoconazole, itraconazole): May significantly increase mobocertinib plasma concentrations; concomitant use is contraindicated.

2.  Moderate CYP3A Inhibitors: If concomitant use cannot be avoided, the dose of mobocertinib should be reduced by approximately 50%.

3.  Strong CYP3A Inducers (e.g., rifampin, St. John's wort) and Grapefruit Products: May reduce the efficacy of mobocertinib; their use should be avoided.

4.  QTc-Prolonging Drugs: Concomitant use with drugs known to prolong the QTc interval increases the risk of arrhythmias and should be avoided.

[Use in Specific Populations]

Hepatic Impairment: No dose adjustment is required for patients with mild hepatic impairment; use is not recommended for patients with moderate or severe hepatic impairment. Renal Impairment: No dose adjustment is required for patients with mild to moderate impairment; use is not recommended for patients with severe impairment.

Geriatric Patients (≥65 years): No dose adjustment is required; however, the incidence of adverse reactions may be higher in this population.

Children and Adolescents: Safety and efficacy have not been established.

Pregnant and Lactating Women: Based on its mechanism of action, this drug may cause fetal harm; therefore, it is contraindicated. Effective contraception must be used during treatment and for at least 1 month after the last dose (for women) or 1 week after the last dose (for men). Breastfeeding is not recommended during treatment and for at least 1 week after the last dose.

[Storage]

Store at room temperature (20–25°C).

Keep out of reach of children.

[Important Information and Updates]

Core Value: Mobocertinib is the first targeted therapy specifically designed for EGFR exon 20 insertion mutations—mutations for which traditional EGFR-TKIs (such as gefitinib and osimertinib) have demonstrated limited efficacy—thereby providing a crucial treatment option for this patient population.

This package insert integrates information from various authoritative drug regulatory agencies and medical centers. It is intended to serve as a comprehensive reference but does not substitute for the prescription and guidance of a qualified physician. All treatment decisions must be made by an oncologist based on the specific circumstances of each individual patient.

Product Specifications

Product Name: Mobocertinib Succinate Capsules (Mobocertinib) — 40 mg × 60 Capsules/Box (Moboxen)

Generic Name: Mobocertinib Succinate Capsules

Active Ingredient: Mobocertinib Succinate

Dosage Form: Hard Capsules

Specification: 40 mg/capsule; 60 capsules/box

Manufacturer: Everest Pharma Ltd (Bangladesh)

Indications: Indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations, whose disease has progressed during or after platinum-based chemotherapy. Prior to use, the presence of the mutation must be confirmed using a validated testing method.

Dosage and Administration: Recommended Dose: 160 mg (four 40 mg capsules) taken orally once daily.

Administration Method: May be taken with food or on an empty stomach. The capsules should be swallowed whole; they must not be opened, chewed, or dissolved.

Management of Missed Doses/Vomiting: If a dose is missed by more than 6 hours, or if vomiting occurs after administration, the missed dose should not be taken; instead, the medication should be taken as usual at the scheduled time on the following day.

Dosage Adjustment: Adjustments are made based on the severity of adverse reactions. The table below outlines the primary dosage adjustment regimen:

Adjustment Step: Dosage Regimen

Starting Dose: 160 mg once daily

First Dose Reduction: 120 mg once daily

Second Dose Reduction: 80 mg once daily