Exkivity

About Mobocertinib

• Mobocertinib, marketed under the brand name Exkivity, is a prescription medication indicated for adults with non-small cell lung cancer (NSCLC) that has metastasized and cannot be surgically removed. 
• It is specifically designed for patients with a certain abnormality in the epidermal growth factor receptor (EGFR) gene, and whose disease has progressed despite undergoing or after platinum-containing chemotherapy. 
• Mobocertinib belongs to the class of small molecule tyrosine kinase inhibitors, structurally akin to osimertinib but distinct due to an additional isopropyl ester group. Its primary molecular target is the EGFR-bearing mutations in the exon 20 region. 
• Functioning as an irreversible kinase inhibitor, Mobocertinib forms a covalent bond with cysteine 797 in the EGFR active site, leading to sustained inhibition of EGFR enzymatic activity. 
• This irreversible binding enhances its potency through higher affinity binding, prolonged EGFR kinase activity inhibition, and increased overall selectivity. 
• Mobocertinib achieved FDA approval for medical use in the United States in September 2021, representing a groundbreaking oral treatment specifically addressing EGFR Exon20 insertion mutations.

Strength: 

Exkivity capsule is available in the strength of 40 mg. 

Recommended Dosage:

Exkivity can be taken with or without food, emphasizing consistency by taking it at the same time daily. Capsules should be swallowed whole, and under no circumstances should they be opened, chewed, or dissolved. Your healthcare provider has the authority to modify your dosage, temporarily halt, or permanently discontinue your Exkivity treatment if specific side effects manifest.

• The recommended dosage for Exkivity is 160 mg administered orally once daily, to be continued until disease progression or the emergence of unacceptable toxicity. 
• If a dose is missed by more than 6 hours, it is advised to skip the missed dose and resume the regular schedule with the next dose the following day. 
• If a dose is vomited, an additional dose should not be taken, and the next prescribed dose should be taken on the subsequent day as instructed.

Important:

Prior to commencing the Exkivity capsule, promptly notify your doctor of any adverse reactions. If you observe unusual symptoms throughout the treatment, consult your doctor immediately. Disclose details of pre-existing health conditions, ensuring comprehensive information for the safe administration of the medication. Open communication about your health is paramount for personalized care and addressing any concerns that may arise during the treatment process. Additionally, make sure to inform your doctor about any current medications to avoid potential interactions, especially for individuals with pre-existing conditions, ensuring comprehensive care and minimizing any associated risks.

Warnings & Precautions

• Monitor patients for signs of Interstitial Lung Disease (ILD)/Pneumonitis, assessing for new or worsening respiratory symptoms. 
• If ILD/pneumonitis is suspected, promptly suspend Exkivity and discontinue permanently upon confirmation. 
• Evaluate cardiac function, specifically left ventricular ejection fraction, before and during treatment to detect potential cardiac toxicity. 
• Adjust the dosage based on severity, with considerations for withholding, resuming at a reduced dose, or permanent discontinuation. 
• Effectively manage diarrhea to prevent dehydration or electrolyte imbalance by monitoring electrolytes, initiating antidiarrheal agents, and advising increased fluid intake. 
• For life-threatening heart rate-corrected QT (QTc) prolongation, conduct baseline and periodic monitoring of QTc and electrolytes, especially in patients with risk factors. 
• Refrain from concurrent use of drugs known to prolong QTc interval and strong or moderate CYP3A inhibitors. 
• Adjust Exkivity dosage in the presence of moderate CYP3A inhibitors. 
• Furthermore, avoid simultaneous administration with strong or moderate CYP3A inducers. Modify Exkivity dosage based on the severity of QTc prolongation.
• Patients should refrain from consuming grapefruit or grapefruit juice while undergoing Exkivity treatment, as it has the potential to elevate the concentration of the medication in the bloodstream.

Common Exkivity Side Effects:

• Diarrhea
• Rash
• Nausea
• Stomatitis (inflammation of the mouth)
• Vomiting
• Decreased appetite
• Paronychia (infection around the fingernails or toenails)
• Fatigue
• Constipation 
• Weight loss
• Dry skin
• Musculoskeletal pain
• Decreased lymphocytes
• Increased amylase
• Increased lipase
• Decreased potassium
• Decreased hemoglobin
• Increased creatinine
• Decreased magnesium

Use in Specific Population

• Due to its mechanism of action and observed effects in animal studies, Exkivity capsules has the potential to cause harm to a developing fetus if administered to pregnant women. Verify pregnancy status in females of reproductive potential before starting Exkivity.
• There are no available data on the presence of mobocertinib or its metabolites in human milk or their impact on the breastfed child or milk production. 
• Due to the potential for serious adverse reactions in breastfed children, women are advised not to breastfeed during Exkivity treatment and for one week after the last dose. 
• Advise females of reproductive potential to use effective non-hormonal contraception during Exkivity treatment and for one month after the last dose. Exkivity may render hormonal contraceptives ineffective. 
• Advise males with female partners of reproductive potential to use effective contraception during Exkivity treatment and for one week after the last dose. 
• Based on animal studies, Exkivity may impair fertility in males and females of reproductive potential. The safety and effectiveness of Exkivity in pediatric patients have not been established. 
• No overall difference in effectiveness was observed between patients aged 65 and older and younger patients. 
• For patients with mild to moderate renal impairment, no dosage adjustment of Exkivity is deemed necessary. However, the recommended dosage of Exkivity has not been defined for those with severe renal impairment. 
• Similarly, for individuals with mild or moderate hepatic impairment, no dosage adjustment of Exkivity is suggested, while the recommended dosage for those with severe hepatic impairment has not been established. 

Storage and Handling

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). Do not freeze the medicine. Keep the medicine away from pets and children. 

• Bottle of 90 capsules 
• Bottle of 120 capsules