Abrocitinib
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Boxed warning
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS (MACE), and THROMBOSIS See full prescribing information for complete boxed warning. • Increased risk of serious bacterial, fungal, viral and opportunistic infections leading to hospitalization or death, including tuberculosis (TB). Discontinue treatment with CIBINQO if serious or opportunistic infection occurs. Test for latent TB before and during therapy; treat latent TB prior to use. Monitor all patients for active TB during treatment, even patients with initial negative latent TB test.
( 5.1 ) • Higher rate of all-cause mortality, including sudden cardiovascular death, with another JAK inhibitor vs. TNF blockers in rheumatoid arthritis (RA) patients. CIBINQO is not approved for use in RA patients. ( 5.2 ) • Malignancies have occurred with CIBINQO. Higher rate of lymphomas and lung cancers with another JAK inhibitor vs. TNF blockers in RA patients. ( 5.3 ) • MACE has occurred with CIBINQO. Higher rate of MACE (defined as cardiovascular death, myocardial infarction, and stroke) with another JAK inhibitor vs. TNF blockers in RA patients. ( 5.4 ) • Thrombosis has occurred with CIBINQO.
Increased incidence of pulmonary embolism, venous and arterial thrombosis with another JAK inhibitor vs. TNF blockers. ( 5.5 ) Serious Infections Patients treated with CIBINQO may be at increased risk for developing serious infections that may lead to hospitalization or death. The most frequent serious infections reported with CIBINQO were herpes simplex, herpes zoster, and pneumonia [see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ] . If a serious or opportunistic infection develops, discontinue CIBINQO and control the infection.
Reported infections from Janus kinase (JAK) inhibitors used to treat inflammatory conditions: • Active tuberculosis, which may present with pulmonary or extrapulmonary disease. Test for latent TB before and during therapy; treat latent TB prior to use. Monitor all patients for active TB during treatment, even patients with initial negative latent TB test. • Invasive fungal infections, including cryptococcosis and pneumocystosis. Patients with invasive fungal infections may present with disseminated, rather than localized, disease. • Bacterial, viral, including herpes zoster, and other infections due to opportunistic pathogens.
Avoid use of CIBINQO in patients with an active, serious infection including localized infections. The risks and…
Janus Kinase Inhibitor
Dosing in kidney impairment
Recommended Dosage in Patients with Renal Impairment or Hepatic Impairment Renal Impairment CIBINQO dosage recommendations for patients with renal impairment are provided in Table 1 [see Use in Specific Populations and Clinical Pharmacology ] . In patients with mild and moderate renal impairment, if an adequate response is not achieved with initial dose, the dose of CIBINQO can be doubled. [See table below.] <15 mL/minute Hepatic Impairment CIBINQO is not recommended for use in patients with severe hepatic impairment (Child-Pugh C).
The recommended dosage in patients with mild (Child-Pugh A) or moderate (Child-Pugh B) hepatic impairment is the same as patients with normal hepatic function [see Use in Specific Populations and Clinical Pharmacology ].
| Renal Impairment Stage | Estimated Glomerular Filtration (eGFR)Glomerular filtration rate was estimated by the Modification of Diet in Renal Disease (MDRD) formula. | Recommended Dosage |
| Mild | 60 – 89 mL/minute | CIBINQO 100 mg once daily |
| Moderate | 30 – 59 mL/minute | CIBINQO 50 mg once daily |
| SevereSevere Renal Impairment and End-Stage Renal Disease include patients on renal replacement therapy. | 15 – 29 mL/minute | Not recommended for use |
| End-Stage Renal Disease (ESRD) | <15 mL/minute |
Dosing in liver impairment
Hepatic Impairment CIBINQO is not recommended in patients with severe (Child-Pugh C) hepatic impairment. In clinical trials, CIBINQO was not evaluated in subjects with severe (Child-Pugh C) hepatic impairment. The recommended dosage in patients with mild (Child-Pugh A) or moderate (Child-Pugh B) hepatic impairment is the same as patients with normal hepatic function and is based on similar combined exposure (AUC inf,u ) of abrocitinib and its two active metabolites, M1 and M2 compared to patients with normal hepatic function [see Clinical Pharmacology ] .
Preparation and administration
Administration Instructions Administer CIBINQO with or without food at approximately the same time each day. Swallow CIBINQO tablets whole with water. Do not crush, split, or chew CIBINQO tablets.
Drug interactions
Check abrocitinib against a medication listLabel text (8 paragraphs)
7 DRUG INTERACTIONS • Strong Inhibitors of CYP2C19 : The recommended dosage is 50 mg once daily or 100 mg once daily for those patients who are not responding to 50 mg once daily. ( 2.5 , 7.1 ) • Moderate to Strong Inhibitors of Both CYP2C19 and CYP2C9, or Strong or Moderate CYP2C19 or CYP2C9 Inducers : Avoid concomitant use. ( 7.1 ) • Certain P-gp Substrates or Certain CYP2C19 Substrates : Monitor or titrate dosage of P-gp substrates or CYP2C19 substrates where small concentration changes may lead to serious or life-threatening toxicities. ( 7.2 )
7.1 Effects of Other Drugs on CIBINQO Table 4 includes drugs with clinically significant drug interactions affecting CIBINQO. Table 4. Clinically Significant Drug Interactions Affecting CIBINQO Strong CYP2C19 Inhibitors Clinical Impact Concomitant use of CIBINQO with strong CYP2C19 inhibitors increases the combined exposure of abrocitinib and its two active metabolites, M1 and M2 which may increase the adverse reactions of CIBINQO [see Clinical Pharmacology (12.3) ]. Intervention Dosage reduction of CIBINQO is recommended when concomitantly used with strong CYP2C19 inhibitors [see Dosage and Administration (2.5) ].
Strong or Moderate Inhibitors of both CYP2C19 and CYP2C9 Clinical Impact Concomitant use of CIBINQO with drugs that are strong or moderate inhibitors of both CYP2C19 and CYP2C9 increases the exposure of abrocitinib and its two active metabolites, M1 and M2 which may increase the adverse reactions of CIBINQO [ Clinical Pharmacology (12.3) ]. Intervention Avoid concomitant use of CIBINQO with drugs that are moderate to strong inhibitors of both CYP2C19 and CYP2C9 .
Strong or Moderate CYP2C19 or CYP2C9 Inducers Clinical Impact Concomitant use of CIBINQO with strong or moderate CYP2C19 or CYP2C9 inducers decreases the combined exposure of abrocitinib and its two active metabolites, M1 and M2, which may result in loss of or reduced clinical response [see Clinical Pharmacology (12.3) ] . Intervention Avoid concomitant use of CIBINQO with strong or moderate CYP2C19 or CYP2C9 inducers.
7.2 Effects of CIBINQO on Other Drugs Table 5 includes clinically significant drug interactions in which CIBINQO affects other drugs. Table 5. Clinically Significant Drug Interactions Affecting Other Drugs Certain P-gp Substrates Clinical Impact Concomitant use of CIBINQO with P-gp substrates increases plasma concentrations of P-gp substrates and may result in potential adverse reactions of the P-gp substrate where minimal increases in the concentration of the P-gp substrate may lead to serious adverse reactions [see Clinical Pharmacology (12.3) ] .
Intervention Monitor appropriately or modify the dosage of the P-gp substrate where small concentration changes may lead to serious or life-threatening toxicities when concomitantly used with CIBINQO. Refer to the Prescribing Information of the P-gp substrate. Certain CYP2C19 Substrates Clinical Impact CIBINQO is a moderate inhibitor of CYP2C19.
Concomitant use of CIBINQO with drugs that are primarily metabolized by the CYP2C19 enzyme may increase the plasma concentrations of the CYP2C19 substrate and may result in potential adverse reactions of the CYP2C19 substrate where minimal increases in the concentration of the CYP2C19 substrate may lead to serious adverse reactions [see Clinical Pharmacology (12.3) ] . Intervention Caution should be exercised when CIBINQO is concomitantly used with drugs that are CYP2C19 sensitive substrates where small concentration changes may lead to serious or life-threatening toxicities.
Antiplatelet Therapy Drugs Clinical Impact Concomitant use of CIBINQO with antiplatelet therapy drugs may increase the risk of bleeding with thrombocytopenia [see Warnings and Precautions (5.5) and Clinical Pharmacology (12.2) ]. Intervention CIBINQO is contraindicated in patients taking antiplatelet drugs, except for low-dose aspirin (≤81 mg daily), during the first 3 months of treatment [see Contraindications (4) ] .
Contraindications
4 CONTRAINDICATIONS CIBINQO is contraindicated in patients taking antiplatelet therapies, except for low-dose aspirin (≤81 mg daily), during the first 3 months of treatment [see Warnings and Precautions (5.7) , Drug Interactions (7.2) , and Clinical Pharmacology (12.2) ]. Antiplatelet therapies except for low-dose aspirin (≤81 mg daily), during the first 3 months of treatment. ( 4 )
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to CIBINQO during pregnancy. Pregnant women exposed to CIBINQO and health care providers are encouraged to call 1-877-311-3770. Risk Summary Available data from pregnancies reported in clinical trials with CIBINQO are not sufficient to establish a drug‑associated risk for major birth defects, miscarriage, or other adverse maternal or fetal outcomes.
In animal reproduction studies, oral administration of abrocitinib to pregnant rats and rabbits during organogenesis at exposure 11 or 4 times the maximum recommended human dose (MRHD) based on AUC comparison, respectively, resulted in maternal dystocia and skeletal variations in rats and no adverse effects in rabbits ( see Data ). The background risks of major birth defects and miscarriage for the indicated population are unknown. All pregnancies carry some risk of birth defects, loss, or other adverse outcomes. The background risks in the U.S. general population of major birth defects and miscarriages are 2–4% and 15–20% of clinically recognized pregnancies, respectively.
Data Animal Data In an embryofetal development study, abrocitinib was administered orally to pregnant rats at doses of 10, 30, or 60 mg/kg/day during the period of organogenesis. No fetal malformations were observed. Abrocitinib increased the incidence of skeletal variations of short 13 th ribs at 30 mg/kg/day (11 times the MRHD based on AUC comparison). Increased embryofetal lethality and additional skeletal variations (cervical arches with reduced ventral processes, thickened ribs, and unossified metatarsals) were noted at 60 mg/kg/day (17 times the MRHD based on AUC comparison).
In an embryofetal development study, abrocitinib was administered orally to pregnant rabbits at doses of 10, 30, or 75 mg/kg/day during the period of organogenesis. No abrocitinib-related maternal or developmental toxicity was noted at doses up to 75 mg/kg/day (4 times the MRHD based on AUC comparison). In a prenatal and postnatal development study, abrocitinib was administered orally to pregnant rats at doses of 10, 30, and 60 mg/kg/day beginning on gestation day 6 and continuing through lactation day 20. Dystocia with prolonged parturition and reduced offspring body weights were noted at 30 mg/kg/day (11 times the MRHD based on AUC comparison).
Postnatal survival was markedly decreased at 60 mg/kg/day (17 times the MRHD based on AUC comparison). No maternal toxicity was observed at 10 mg/kg/day (2.4 times the MRHD based on AUC…
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
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Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
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