Dosing & Uses
Dosage Forms & Strengths
tablets
- 50mg
- 100mg
- 200mg
Atopic Dermatitis
Indicated for refractory moderate-to-severe atopic dermatitis (AD) in patients aged ≥12 years whose disease is not adequately controlled with other systemic therapies or for whom those therapies are inadvisable
100 mg PO qDay
If adequate response not achieved after 12 weeks, consider increasing to 200 mg qDay
Discontinue 200-mg dose if adequate response not achieved
Use with or without topical corticosteroids
Dosage Modifications
CYP2C19 poor metabolizers or coadministration with strong CYP2C19 inhibitors
- 50 mg qDay initially; if adequate response not achieved after 12 weeks, may increase to 100 mg qDay
- Discontinue if inadequate response after dosage increase
Infection
- If serious infection (eg, serious opportunistic infection) develops, interrupt treatment until infection is controlled
- Carefully consider risks and benefits of treatment before reinitiating
Hematologic abnormalities
- Platelet count <50,000/mm3: Discontinue therapy and monitor until platelet count >100,000/mm3
- Absolute lymphocyte count (ALC) <500 cells/mm3: Interrupt therapy; may restart once ALC >500 cells/mm3
- Absolute neutrophil count (ANC) <1000 cells/mm3: Interrupt therapy; may restart once ANC >1000 cells/mm3
- Hemoglobin (Hb) <8 g/dL: Interrupt therapy; may restart once Hb >8 g/dL
Renal impairment
- Mild (eGFR 60-89 mL/min): No dosage adjustment necessary
- Moderate (eGFR 30-59 mL/min): 50 mg qDay initially; may double dose if adequate response not achieved after 12 weeks
- Severe or end-stage renal disease (eGFR <29 mL/min): Not recommended
- Patients on renal replacement therapy: Not studied; not recommended
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dose adjustment required
- Severe (Child-Pugh C): Not recommended
Dosing Considerations
Before initiating
- Test for tuberculosis (TB) before initiating; initiate antitubercular treatment for previously untreated latent TB or active TB before initiating treatment
- Screen viral hepatitis in accordance with clinical guidelines
- Update immunizations according to current immunization guidelines
- CBC at baseline, 4 weeks after initiating, and 4 weeks after dosing; may extend for patients on chronic therapy who develop hematologic abnormalities
Not recommended for patients with the following
- ALC <500 cells/mm3, ANC <1000 cell/mm3, or Hb <8 g/dL
- Active hepatitis B or hepatitis C
Limitations of use
- Not recommended for use in combination with other Janus kinase (JAK) inhibitors, with biologic immunomodulators, or with other immunosuppressants
Dosage Forms & Strengths
tablets
- 50mg
- 100mg
- 200mg
Atopic Dermatitis
Indicated for refractory moderate-to-severe atopic dermatitis (AD) in patients aged ≥12 years whose disease is not adequately controlled with other systemic therapies or for whom those therapies are inadvisable
<12 years: Safety and efficacy not established
≥12 years
- 100 mg PO qDay
- If adequate response not achieved after 12 weeks, consider increasing to 200 mg qDay
- Discontinue 200-mg dose if adequate response not achieved
- Use with or without topical corticosteroids
Dosage Modifications
CYP2C19 poor metabolizers or coadministration with strong CYP2C19 inhibitors
- 50 mg qDay initially; if adequate response not achieved after 12 weeks, may increase to 100 mg qDay
- Discontinue if inadequate response after dosage increase
Infection
- If serious infection (eg, serious opportunistic infection) develops, interrupt treatment until infection is controlled
- Carefully consider risks and benefits of treatment before reinitiating
Hematologic abnormalities
- Platelet count <50,000/mm3: Discontinue therapy and monitor until platelet count >100,000/mm3
- Absolute lymphocyte count (ALC) <500 cells/mm3: Interrupt therapy; may restart once ALC >500 cells/mm3
- Absolute neutrophil count (ANC) <1000 cells/mm3: Interrupt therapy; may restart once ANC >1000 cells/mm3
- Hemoglobin (Hb) <8 g/dL: Interrupt therapy; may restart once Hb >8 g/dL
Renal impairment
- Mild (eGFR 60-89 mL/min): No dosage adjustment necessary
- Moderate (eGFR 30-59 mL/min): 50 mg qDay initially; may double dose if adequate response not achieved after 12 weeks
- Severe or end-stage renal disease (eGFR <29 mL/min): Not recommended
- Patients on renal replacement therapy: Not studied; not recommended
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dose adjustment required
- Severe (Child-Pugh C): Not recommended
Dosing Considerations
Before initiating
- Test for tuberculosis (TB) before initiating; initiate antitubercular treatment for previously untreated latent TB or active TB before initiating treatment
- Screen viral hepatitis in accordance with clinical guidelines
- Update immunizations according to current immunization guidelines
- CBC at baseline, 4 weeks after initiating, and 4 weeks after dosing; may extend for patients on chronic therapy who develop hematologic abnormalities
Not recommended for patients with the following
- ALC <500 cells/mm3, ANC <1000 cell/mm3, or Hb <8 g/dL
- Active hepatitis B or hepatitis C
Limitations of use
- Not recommended for use in combination with other Janus kinase (JAK) inhibitors, with biologic immunomodulators, or with other immunosuppressants
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (14)
- abciximab
abrocitinib and abciximab both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- anagrelide
abrocitinib and anagrelide both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- aspirin
abrocitinib and aspirin both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- cangrelor
abrocitinib and cangrelor both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- cilostazol
abrocitinib and cilostazol both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- clopidogrel
abrocitinib and clopidogrel both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- dipyridamole
abrocitinib and dipyridamole both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- eptifibatide
abrocitinib and eptifibatide both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- prasugrel
abrocitinib and prasugrel both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- ticagrelor
abrocitinib and ticagrelor both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- ticlopidine
abrocitinib and ticlopidine both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- tirofiban
abrocitinib and tirofiban both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
- upadacitinib
abrocitinib, upadacitinib. Either increases effects of the other by immunosuppressive effects; risk of infection. Contraindicated.
- vorapaxar
abrocitinib and vorapaxar both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.
Serious - Use Alternative (41)
- adenovirus types 4 and 7 live, oral
abrocitinib decreases effects of adenovirus types 4 and 7 live, oral by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- axicabtagene ciloleucel
abrocitinib, axicabtagene ciloleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- BCG vaccine live
abrocitinib decreases effects of BCG vaccine live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- brexucabtagene autoleucel
abrocitinib, brexucabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of abrocitinib by increasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are strong inducers of CYP2C19 or CYP2C9 decreases the combined exposure of abrocitinib and its active metabolites, resulting in loss of or reduced clinical response.
- cholera vaccine
abrocitinib decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- ciltacabtagene autoleucel
abrocitinib, ciltacabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- delavirdine
delavirdine will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- dengue vaccine
abrocitinib decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- Ebola Zaire vaccine
abrocitinib decreases effects of Ebola Zaire vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- efavirenz
efavirenz will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- etravirine
etravirine will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- fluconazole
fluconazole will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- fosphenytoin
fosphenytoin will decrease the level or effect of abrocitinib by increasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are strong inducers of CYP2C19 or CYP2C9 decreases the combined exposure of abrocitinib and its active metabolites, resulting in loss of or reduced clinical response.
- gemfibrozil
gemfibrozil will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- idecabtagene vicleucel
abrocitinib, idecabtagene vicleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- influenza virus vaccine quadrivalent, intranasal
abrocitinib decreases effects of influenza virus vaccine quadrivalent, intranasal by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- ketoconazole
ketoconazole will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- levoketoconazole
levoketoconazole will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- lisocabtagene maraleucel
abrocitinib, lisocabtagene maraleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- measles (rubeola) vaccine
abrocitinib decreases effects of measles (rubeola) vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- measles mumps and rubella vaccine, live
abrocitinib decreases effects of measles mumps and rubella vaccine, live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- measles, mumps, rubella and varicella vaccine, live
abrocitinib decreases effects of measles, mumps, rubella and varicella vaccine, live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- nicardipine
nicardipine will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- omeprazole
omeprazole will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- phenytoin
phenytoin will decrease the level or effect of abrocitinib by increasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are strong inducers of CYP2C19 or CYP2C9 decreases the combined exposure of abrocitinib and its active metabolites, resulting in loss of or reduced clinical response.
- poliovirus vaccine live oral trivalent
abrocitinib decreases effects of poliovirus vaccine live oral trivalent by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- rifampin
rifampin will decrease the level or effect of abrocitinib by increasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are strong inducers of CYP2C19 or CYP2C9 decreases the combined exposure of abrocitinib and its active metabolites, resulting in loss of or reduced clinical response.
- rotavirus oral vaccine, live
abrocitinib decreases effects of rotavirus oral vaccine, live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- rubella vaccine
abrocitinib decreases effects of rubella vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- rucaparib
rucaparib will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- smallpox (vaccinia) and monkeypox vaccine, live, nonreplicating
abrocitinib decreases effects of smallpox (vaccinia) vaccine, attenuated by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- smallpox (vaccinia) vaccine, attenuated
abrocitinib decreases effects of smallpox (vaccinia) vaccine, attenuated by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- smallpox (vaccinia) vaccine, live
abrocitinib decreases effects of smallpox (vaccinia) vaccine, live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- tisagenlecleucel
abrocitinib, tisagenlecleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- typhoid polysaccharide vaccine
abrocitinib decreases effects of typhoid polysaccharide vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- typhoid vaccine live
abrocitinib decreases effects of typhoid vaccine live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- varicella virus vaccine live
abrocitinib decreases effects of varicella virus vaccine live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- voriconazole
voriconazole will increase the level or effect of abrocitinib by decreasing metabolism. Avoid or Use Alternate Drug. Abrocitinib is a CYP2C9 and CYP2C19 substrate. Drugs that are moderate-to-strong inhibitors of both CYP2C9 and CYP2C19 increase systemic exposure of abrocitinib and its active metabolites, which may increase adverse effects.
- yellow fever vaccine
abrocitinib decreases effects of yellow fever vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
- zoster vaccine live
abrocitinib decreases effects of zoster vaccine live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Administration of live vaccines is not recommended during abrocitinib treatment and immediately before or after treatment.
Monitor Closely (13)
- chloramphenicol
chloramphenicol will increase the level or effect of abrocitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Start abrocitinib 50 mg qDay when coadministered with CYP2C19 inhibitors. If adequate response not achieved after 12 weeks, may increase to 100 mg qDay. Discontinue if inadequate response after dosage increase.
- clonidine
abrocitinib will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor and titrate dose of P-gp substrate appropriately.
- colchicine
abrocitinib will increase the level or effect of colchicine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor and titrate dose of P-gp substrate appropriately.
- digoxin
abrocitinib will increase the level or effect of digoxin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor and titrate dose of P-gp substrate appropriately.
- fluvoxamine
fluvoxamine will increase the level or effect of abrocitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Start abrocitinib 50 mg qDay when coadministered with CYP2C19 inhibitors. If adequate response not achieved after 12 weeks, may increase to 100 mg qDay. Discontinue if inadequate response after dosage increase.
- isoniazid
isoniazid will increase the level or effect of abrocitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Start abrocitinib 50 mg qDay when coadministered with CYP2C19 inhibitors. If adequate response not achieved after 12 weeks, may increase to 100 mg qDay. Discontinue if inadequate response after dosage increase.
- modafinil
modafinil will increase the level or effect of abrocitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Start abrocitinib 50 mg qDay when coadministered with CYP2C19 inhibitors. If adequate response not achieved after 12 weeks, may increase to 100 mg qDay. Discontinue if inadequate response after dosage increase.
- omeprazole
omeprazole will increase the level or effect of abrocitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Start abrocitinib 50 mg qDay when coadministered with CYP2C19 inhibitors. If adequate response not achieved after 12 weeks, may increase to 100 mg qDay. Discontinue if inadequate response after dosage increase.
- sirolimus
abrocitinib will increase the level or effect of sirolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor and titrate dose of P-gp substrate appropriately.
- sitaxentan
sitaxentan will increase the level or effect of abrocitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Start abrocitinib 50 mg qDay when coadministered with CYP2C19 inhibitors. If adequate response not achieved after 12 weeks, may increase to 100 mg qDay. Discontinue if inadequate response after dosage increase.
- temsirolimus
abrocitinib will increase the level or effect of temsirolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor and titrate dose of P-gp substrate appropriately.
- ticlopidine
ticlopidine will increase the level or effect of abrocitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Start abrocitinib 50 mg qDay when coadministered with CYP2C19 inhibitors. If adequate response not achieved after 12 weeks, may increase to 100 mg qDay. Discontinue if inadequate response after dosage increase.
- ublituximab
ublituximab and abrocitinib both increase immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Owing to potential additive immunosuppressive effects, consider duration of effect and mechanism of action of these therapies if coadministered
Minor (0)
Adverse Effects
>10%
Nausea (6-14.5%)
Nasopharyngitis (8.7-12.4%)
1-10%
Headache (6-7.8%)
Acne (1.6-4.7%)
Herpes simplex (3.3-4.2%)
Vomiting (1.5-3.2%)
Increased blood creatinine phosphokinase (2.3-2.9%)
Dizziness (1.8-2.9%)
Urinary tract infection (1.7-2.2%)
Upper abdominal pain (0.6-1.9%)
Fatigue (1.3-1.6%)
Impetigo (0.5-1.5%)
Thrombocytopenia (1.5%)
Oropharyngeal pain (1-1.4%)
Gastroenteritis (1.1-1.3%)
Influenza (1.1-1.2%)
Hypertension (0.8-1.2%)
Abdominal discomfort (0.5-1.2%)
Herpes zoster (0.3-1.2%)
Contact dermatitis (0.5-1.1%)
Warnings
Black Box Warnings
Serious infection
- Increases risk for developing serious infections that may lead to hospitalization or death
- Most common serious infections reported were herpes simplex, herpes zoster, and pneumonia
- If serious opportunistic infection develops, discontinue therapy until infection controlled
- Avoid use with an active serious infection, including localized infections; carefully consider risks and benefits before initiating therapy in patients with chronic or recurrent infection
- Closely monitor for signs and symptoms of infection during and after treatment, including possible development of tuberculosis (TB) in patients who tested negative for latent TB infection before initiating therapy
-
Reported infections include
- Active TB, which may present with pulmonary or extrapulmonary disease; test for latent TB before use and during therapy; consider treating latent infection before use
- Invasive fungal infections, including cryptococcosis and pneumocystosis
- Bacterial, viral (including herpes zoster), and other infections due to opportunistic pathogens
Mortality
- Not approved for rheumatoid arthritis (RA)
- Patients with RA aged ≥50 years with at least 1 cardiovascular risk factor, in a comparison of another Janus kinase (JAK) inhibitor with TNF blockers, showed a higher rate of all-cause mortality, including sudden cardiovascular death, with the JAK inhibitor
Malignancies
- Lymphoma and other malignancies reported
- Higher rate of malignancies (excluding nonmelanoma skin cancer) observed
- Current or past smokers are at additional increased risk
Major adverse cardiovascular events (MACE)
- In patients with RA aged ≥50 years with at least 1 cardiovascular risk factor treated with another JAK inhibitor, a higher rate of MACE (defined as cardiovascular death, myocardial infarction, and stroke), was observed
- Patients who are current or past smokers are at additional increased risk
- Discontinue therapy if myocardial infarction or stroke occurs
Thrombosis
- Thrombosis, including deep venous thrombosis (DVT), pulmonary embolism (PE), and arterial thrombosis reported
- Many of these adverse events were serious, and some resulted in death
- Avoid therapy in patients at risk
- If symptoms of thrombosis occur, discontinue therapy, and treat appropriately
Contraindications
Concomitant antiplatelet therapies, except for low-dose aspirin (≤81 mg qDay), during initial 3 months of treatment
Cautions
Malignancies reported; consider risks and benefits of treatment before initiating in patients with known malignancy, other than previously treated nonmelanoma skin cancer; screen for malignancies during treatment according to guidelines
Perform periodic skin examination for patients who are at increased risk for skin cancer; limit exposure to sun and ultraviolet (UV) light by wearing protective clothing and using broad-spectrum sunscreen
Higher rate of major adverse cardiovascular events (MACE; defined as cardiovascular death, myocardial infarction, and stroke) reported with another JAK inhibitor vs TNF blockers in RA patients
Thrombosis reported, including deep vein thrombosis (DVT), pulmonary embolism (PE), and arterial thrombosis; avoid therapy in patients who may be at increased risk of thrombosis
In patients with rheumatoid arthritis (RA) aged ≥50 years with at least 1 cardiovascular risk factor, a higher rate of all-cause mortality, including sudden cardiovascular death, was observed; not approved for RA
May cause neutropenia, lymphopenia, anemia, elevated lipids, or elevated liver enzymes; monitor for abnormal laboratory values, and assess the need to interrupt dosing
Serious and fatal infections
- Serious and fatal infections reported
- Most frequent infections reported included herpes zoster, herpes simplex, and pneumonia
- Avoid use in patients with active serious infection, including localized infections
- Closely monitor for developing signs and symptoms of infection during and after treatment
- Discontinue therapy if serious or opportunistic infection develops
- Initiate prompt and complete diagnostic testing appropriate for immunocompromised patient if new infection develops; initiate appropriate antimicrobial therapy
- Carefully consider risk and benefits of treatment before restarting
- Screen patients for opportunistic infections (eg, TB), and treat according to guidelines
-
Tuberculosis (TB)
- Not recommended for use in patients with active TB
- Before initiating, start preventive therapy for latent TB in newly diagnosed patients with latent TB, patients with previously untreated latent TB, or patients with a negative test for latent TB but who are at high risk for TB infection
- Monitor for developing signs and symptoms of TB
-
Viral reactivation
- Viral reactivation, including cases of herpes virus reactivation (eg, herpes zoster) and hepatitis B virus reactivation, were reported
- If herpes zoster develops, consider temporarily interrupting therapy until episode resolves
- Screen for viral hepatitis and monitor for reactivation in accordance with clinical guidelines before starting and during therapy
-
Consider risks and benefits of treatment before initiating in the following patients
- With chronic or recurrent infection
- Who have been exposed to TB
- With history of serious or opportunistic infection
- Who have resided or traveled in areas of endemic tuberculosis or endemic mycoses
- With underlying conditions that may predispose them to infection
Drug interaction overview
- Substrate of CYP2C9 and CYP2C19
- Inhibitor of P-glycoprotein (P-gp)
-
Strong CYP2C19 inhibitors
- Reduce abrocitinib dose
- Strong CYP2C19 inhibitors increase systemic exposure of abrocitinib and its metabolites
-
Moderate-to-strong inhibitors of both CYP2C9 and CYP2C19
- Avoid coadministration
- Moderate-to-strong CYP2C9 and CYP2C19 inhibitors increase systemic exposure and adverse reactions of abrocitinib and its metabolites
-
Strong CYP2C9 or CYP2C19 inducers
- Avoid coadministration
- Strong CYP2C9 or CYP2C19 inducers decrease systemic exposure of abrocitinib and its metabolites
-
Sensitive P-gp substrates
- Monitor and titrate dose of P-gp substrates accordingly
- Abrocitinib increases plasma concentrations and adverse reactions of P-gp substrates where small concentration changes may lead to serious or life-threatening toxicities (eg, digoxin)
-
Antiplatelet therapy
- Contraindicated, except for low-dose aspirin (≤81 mg qDay), during initial 3 months of treatment
- Abrocitinib may increase bleeding risk with thrombocytopenia
-
Vaccines
- Use of live attenuated vaccines during or immediately before initiating is not recommended
- Before initiating, assess vaccination history, including prophylactic zoster vaccinations
- Ensure vaccinations are current before initiating
Pregnancy & Lactation
Pregnancy
Data are insufficient to evaluate drug-associated risk for major birth defects, miscarriage, or other adverse maternal or fetal outcomes
Pregnancy exposure registry
- Monitors outcomes in females exposed to drug during pregnancy
- Contact 1-877-311-3770 to register
Infertility
- May impair female fertility
- Impaired fertility in female rats was reversible 1 month after discontinuing abrocitinib
Animal data
- No fetal malformations were observed when abrocitinib was administered orally to pregnant rats at doses of 10, 30, or 60 mg/kg/day during organogenesis
- Abrocitinib increased the incidence of skeletal variations of short 13th ribs at 30 mg/kg/day (14x the maximum recommended human dose)
- 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
Lactation
No data available on presence in human milk, effects on breastfed infants, or effects on milk production
Abrocitinib secreted in milk of lactating rats
If a drug is present in animal milk, it is likely the drug will be present in human milk
Advise patients that breastfeeding is not recommended during treatment and for 1 days (~5-6 half-lives) after the last dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Janus kinase (JAK) inhibitor; reversibly inhibits Janus kinase-1 (JAK1) by blocking adenosine triphosphate binding site
JAK-1 is essential for certain cytokines to elicit signals from various interleukins, cardiotrophin, neurotrophin, and interferons that are involved in inflammatory processes
Absorption
Peak plasma time: 1 hr
Bioavailability: 60%
Steady-state reached at 48 hr
Effect of food
- High-fat, high-calorie meal (916 calories [55% fat, 29% carbohydrates, and 16% protein]): No clinically relevant effect on AUC or peak plasma concentration
Distribution
Vd: 100 L
Protein bound
- Abrocitinib: 64%
- M1 metabolite: 37%
- M2 metabolite: 29%
Metabolism
Metabolism is mediated by CYP2C19 (~53%), CYP2C9 (~30%), CYP3A4 (~11%) and CYP2B6 (~6%)
Metabolites: M1 (less active) and M2
Elimination
Half-life: 3-5 hr (abrocitinib and metabolites)
Excretion
- Urine: 1% (unchanged)
- Metabolites of abrocitinib, M1 and M2 are excreted predominantly in urine, and are substrates of OAT3 transporter
Pharmacogenomics
CYP2C19 poor metabolizers have little to no CYP2C19 enzyme function compared with CYP2C19 normal metabolizers
After doses of abrocitinib, CYP2C19 poor metabolizers demonstrated dose-normalized AUC values that were 2.3-fold higher when compared with CYP2C19 normal metabolizer
Administration
Oral Administration
Take orally with or without food at approximately the same time each day
Swallow tablet whole; do not split, crush, or chew
Missed dose
- ≥12 hr before next dose: Administer as soon as possible
- <12 hr before next dose: Skip missed dose; resume dosing at the next scheduled time
Storage
Store at 2-25ºC (36-77ºF)
Store in original bottle to protect from moisture
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
