Cibinqo

About Abrocitinib

• Abrocitinib, marketed under the brand name Cibinqo, is a medication designed to treat atopic dermatitis (eczema). 
• Abrocitinib was developed by Pfizer, it falls into the category of Janus kinase inhibitors and is administered orally. 
• The European Union approved for medical use of Abrocitinib in December 2021, followed by FDA approval in the United States on January 14, 2022. 
• Cibinqo, a Janus kinase (JAK) inhibitor, is prescribed for adults with refractory, moderate-to-severe atopic dermatitis. It is recommended when other systemic drug products, including biologics, are ineffective in controlling the disease or when the use of those therapies is inadvisable.
• Abrocitinib functions by reducing the activity of the immune system. In terms of its mechanism, Abrocitinib reversibly inhibits JAK1 by obstructing the adenosine triphosphate (ATP) binding site. 
• Notably, it exhibits selectivity for JAK1 over JAK2 (28-fold), JAK3 (>340-fold), and tyrosine kinase (TYK) 2 (43-fold) in a cell-free isolated enzyme assay, as well as within the broader kinome. 
• The current understanding of how the inhibition of specific JAK enzymes contributes to therapeutic effectiveness is limited. Both the parent compound and the active metabolites demonstrate inhibition of JAK1 activity in vitro with comparable levels of selectivity.
• Atopic dermatitis, commonly known as eczema, is a skin condition characterized by dry, itchy, and inflamed skin. 

Strength: 

Cibinqo tablets are available in the strength of 50 mg, 100 mg, and 200 mg

Recommended Dosage:

Before starting Cibinqo, evaluate patients for active tuberculosis (TB) infection, and initiate preventive therapy for latent TB in those at high risk. Screen for active hepatitis B or C, as Cibinqo initiation is not recommended in such cases. Conduct a complete blood count (CBC) and avoid initiation if the platelet count is <150,000/mm3, absolute lymphocyte count is <500/mm3, absolute neutrophil count is <1,000/mm3, or hemoglobin value is <8 g/dL. Administer necessary immunizations, including herpes zoster vaccinations, based on current guidelines before initiating Cibinqo.

• The recommended dosage of Cibinqo Pfizer is 100 mg orally once daily. If there’s an inadequate response after 12 weeks, consider increasing the dosage to 200 mg orally once daily. 
• Discontinue therapy if an inadequate response persists after the dosage is raised to 200 mg once daily. 
• Cibinqo can be used with or without topical corticosteroids. Follow your healthcare provider’s instructions precisely. 
• Take Cibinqo once daily at the same time, swallowing the tablets whole with water,  do not split, crush, or chew them. You can take Cibinqo with or without food. It can be used alongside prescribed topical medicines for atopic dermatitis. 
• In case of a missed dose, take it as soon as possible, skip it if it’s less than 12 hours before the next scheduled dose, and resume the usual schedule.

Important:

In the initial three months of Cibinqo treatment, avoid concurrent use with other medications preventing blood clots. If prescribed by your healthcare provider, you may take low-dose aspirin up to 81 mg daily during this period.

Warnings & Precautions

• Cibinqo poses an increased risk of severe bacterial, fungal, viral, and opportunistic infections, including tuberculosis (TB), potentially leading to hospitalization or death. 
• Discontinue treatment with Cibinqo in the event of a serious or opportunistic infection, and initiate latent TB treatment if necessary. Monitor all patients for active TB during treatment. 
• Notably, another JAK inhibitor, unrelated to Cibinqo, exhibited a higher all-cause mortality rate, including sudden cardiovascular death, compared to TNF blockers in rheumatoid arthritis (RA) patients. 
• However, it’s important to clarify that Cibinqo is not approved for use in RA. Instances of malignancies, particularly lymphomas and lung cancers, have been reported with Cibinqo use. 
• Additionally, another JAK inhibitor demonstrated a higher incidence of major adverse cardiovascular events (MACE) compared to TNF blockers in RA patients. 
• Thrombosis, including pulmonary embolism, venous, and arterial thrombosis, has occurred with Cibinqo. 
• Increased vigilance is advised, especially in individuals with infections, a history of smoking, heart issues, kidney or liver problems, low platelet or white blood cell counts, eye problems, or recent immunizations. 
• Users of Cibinqo should avoid live vaccines, and regular laboratory monitoring is recommended for potential changes in platelets, lymphocytes, and lipids.

Common Cibinqo Side Effects:

• Cytokine release syndrome (CRS)
• Back pain
• Burning/crawling/itching/numbness/tingling
• Constipation
• Difficulty moving
• Joint pain/swelling
• Skin lightening
• Hair loss/thinning
• Muscle aches/cramps/pain/stiffness
• Night sweats
• Arm/leg pain
• Runny nose
• Shivering
• Sore throat
• Trouble sleeping
• Rash
• Pyrexia (fever)
• Pruritus (itching)
• Fatigue
• Nausea & vomiting
• Chills
• Abdominal pain
• Edema (swelling)
• Hypotension (low blood pressure)
• Dry skin
• Headache
• Dizziness
• Urinary tract infection
• Difficulty breathing
• Seizures

Use in Specific Population

Pregnancy: Insufficient data from clinical trials are available to determine the drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes with Cibinqo during pregnancies. 

Breastfeeding: No information exists regarding the presence of abrocitinib in human milk, its impact on the breastfed infant, or its effects on milk production. Lactating rats demonstrated the secretion of abrocitinib in their milk, suggesting potential transmission to human milk. Given the severe adverse effects observed in adults, including serious infections, malignancies, and thrombosis, women are advised against breastfeeding during Cibinqo treatment and for one day after the final dose (approximately 5-6 elimination half-lives). 

Pediatric patients: The safety and efficacy of Cibinqo have not been established in pediatric patients.

Kidney Disease: Cibinqo is not recommended for individuals with severe kidney impairment and end-stage kidney disease (ESRD), including those undergoing kidney replacement therapy. For patients with moderate kidney impairment, a dosage reduction is advised. No dosage adjustment is necessary for patients with mild kidney impairment (eGFR 60-89 mL/min). Cibinqo has not undergone study in patients on kidney replacement therapy. 

Liver Disease: Do not use Cibinqo in patients with severe liver impairment (Child-Pugh C).

Storage and Handling

• Store Cibinqo at room temperature between 68°F to 77°F (20°C to 25°C).
• Avoid freezing the tablets. 
• Store Cibinqo in the original pack. 
• Protect Cibinqo from direct light exposure. 
• Keep the medicine away from pets and children.