1 / 1

Mobocertinib(Exkivity)

Acetylcysteine Injection, FLUIMUCIL, Acetylcysteine InjectionAcetylcysteine Injection, FLUIMUCIL, Acetylcysteine InjectionAcetylcysteine Injection, FLUIMUCIL, Acetylcysteine Injection

Reference price:

Manufacturer:

Formulation:

CAPSULE

Validity period:

Not specified in the provided excerpts.

Reminder: The outer packaging is for reference only, please purchase and use under the guidance of a pharmacist. For read by medical and pharmaceutical professionals only.

EXKIVITY (mobocertinib) is an orally administered kinase inhibitor designed to target specific mutations in the epidermal growth factor receptor (EGFR). Its chemical name is propan-2-yl 2-[5-(acryloylamino)-4-{2-(dimethylamino)ethylamino}-2-methoxyanilino]-4-(1-https://www.google.com/search?q=methyl-1H-indol-3-yl)pyrimidine-5-carboxylate succinate. The drug is supplied as 40 mg capsules for oral use. Mobocertinib functions by irreversibly binding to and inhibiting EGFR exon 20 insertion mutations at concentrations lower than those required to inhibit wild-type (WT) EGFR. This selective inhibition is crucial for its therapeutic effect in the indicated patient population.

The mechanism involves targeting the kinase activity of EGFR, thereby disrupting downstream signaling pathways that promote cell proliferation and survival in cancer cells harboring these specific mutations. In addition to mobocertinib itself, two pharmacologically active metabolites, AP32960 and AP32914, which have similar inhibitory profiles to the parent drug, have been identified in plasma following oral administration. In vitro studies have also shown that mobocertinib can inhibit other EGFR family members (HER2 and HER4) and one additional kinase (BLK) at clinically relevant concentrations. This targeted approach aims to provide a therapeutic benefit for patients with EGFR exon 20 insertion mutation-positive NSCLC.

Generic name

Mobocertinib(Exkivity)

English name

Mobocertinib

Alternative Names

Exkivity

Drug prices

Indications

EXKIVITY is a kinase inhibitor indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations, as detected by an FDA-approved test, whose disease has progressed on or after platinum-based chemotherapy. This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s).

Therapeutic Target

Epidermal Growth Factor Receptor (EGFR) with exon 20 insertion mutations

Active Ingredients

Each capsule contains 40 mg of mobocertinib (equivalent to 48.06 mg mobocertinib succinate).

Dosage form

CAPSULE

specifications

Capsules: 40 mg. Other packaging details (e.g., count per bottle) are not specified in the highlights or initial sections but would be found in "HOW SUPPLIED/STORAGE AND HANDLING".

Description

40 mg capsules, white, size 2, imprinted with “MB788” on the cap and “40mg” on the body in black ink.

Dosage and Administration

Recommended Dosage: 160 mg orally once daily, with or without food, until disease progression or unacceptable toxicity. Swallow capsules whole; do not open, chew, or dissolve.

Miss Dose: If a dose is missed by more than 6 hours, skip the dose and take the next dose the following day at its regularly scheduled time.

Vomited Dose: If a dose is vomited, do not take an additional dose. Take the next dose as prescribed the following day.

Recommended Evaluation Before Initiating: Evaluate QTc and electrolytes (sodium, potassium, calcium, magnesium) and correct abnormalities before starting.

Patient Selection: Select patients based on the presence of EGFR exon 20 insertion mutations detected by an FDA-approved test.

**Dosage Modifications for Adverseeactions:**

Dose Reductions: First reduction to 120 mg once daily, second reduction to 80 mg once daily.

QTc Prolongation: Specific guidance for withholding, resuming at same or reduced dose, or permanent discontinuation based on severity (Grade 2, 3, or 4 Torsades de Pointes).

Interstitial Lung Disease (ILD)/Pneumonitis: Withhold if suspected; permanently discontinue if confirmed.

Decreased Ejection Fraction/Heart Failure: Withhold for Grade 2 decreased ejection fraction. Resume at same or lower dose if recovered within 2 weeks; otherwise, permanently discontinue. Permanently discontinue for ≥Grade 2 heart failure or Grade 3 or 4 decreased ejection fraction.

Diarrhea: Withhold for intolerable/recurrent Grade 2 or Grade 3; resume at same or lower dose. For Grade 4, withhold; resume at next lower dose for first occurrence. Permanently discontinue on recurrence of Grade 4.

Increased Amylase or Lipase: Specific guidance for withholding, resuming at same or reduced dose, or permanent discontinuation based on grade and symptoms. -----Other Adverse Reactions:* Withhold for intolerable/recurrent Grade 2 or Grade 3; resume at same or lower dose. For Grade 4, withhold; resume at next lower dose if recovery within 2 weeks for first occurrence. Permanently discontinue if no recovery within 2 weeks or on recurrence.

Dosage Modifications for Moderate CYP3A Inhibitors: Avoid concomitant use. If unavoidable, reduce EXKIVITY dose by approximately 50% (e.g., 160 mg to 80 mg) and monitor QTc more frequently. Resume prior dose 3-5 elimination half-lives after discontinuing the inhibitor.

Dosage Modifications for Patients with Severe Renal Impairment: Reduce EXKIVITY dose by approximately 50% (e.g., 160 mg to 80 mg) and monitor QTc more frequently (eGFR <30 mL/min/1.73 m²).

CATEGORY NAVIGATION