abrocitinib

Absorption: Well absorbed following oral administration.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP2C19, CYP2C9, CYP3A4, and CYP2B6 isoenzymes into two active metabolites (M1 and M2). 2% of White people, 4% of Black people, and 14% of Asian people have CYP2C19 genotype that results in ↓ metabolism of abrocitinib. Primarily excreted in urine (<1% as unchanged drug).

Half-Life: 3–5 hr.

Time/Action Profile ⬆ ⬇

( plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	<1 hr	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Concurrent use of antiplatelet therapies (excluding low-dose aspirin [≤81 mg/day]) for the 1st 3 mo of treatment;
Active infection;
Platelet count <150,000/mm³, lymphocyte count <500 cells/mm³, ANC <1000 cells/mm³, or hemoglobin level <8 g/dL;
↑risk for thrombosis;
Severe renal impairment or end-stage renal disease;
Severe hepatic impairment;
Lactation: Lactation.

Use Cautiously in:

Patients who are >50 yr old and have ≥1 cardiovascular risk factor (↑ risk of all-cause mortality, cardiovascular death, MI, stroke, and thrombosis);
Chronic or recurrent infection;
Previously exposed to tuberculosis (TB);
History of serious or opportunistic infection;
Resided or traveled in areas of endemic tuberculosis or endemic mycoses;
Underlying conditions that predispose to infection;
Malignancy (other than successfully treated nonmelanoma skin cancer);
Current or previous smoker (↑ risk of malignancy);
Known or suspected CYP2C19 poor metabolizers (↓ dose);
Moderate renal impairment (↓ dose);
OB: Other agents for atopic dermatitis preferred in pregnancy;
Pedi: Children <12 yr (safety and effectiveness not established);
Geri: Older adults may have ↑ risk of lymphopenia, thrombocytopenia, and herpes infection.

Adv. Reactions/Side Effects ⬆ ⬇

CV: CARDIOVASCULAR DEATH, DEEP VEIN THROMBOSIS (DVT), hypertension, MI

Derm: acne, contact dermatitis, impetigo

EENT: nasopharyngitis, retinal detachment

GI: nausea, abdominal pain, oropharyngeal pain, vomiting

Hemat: lymphopenia, thrombocytopenia

Metab: hyperlipidemia

MS: ↑CK

Neuro: dizziness, fatigue, headache, STROKE

Resp: PULMONARY EMBOLISM (PE)

Misc: INFECTION (INCLUDING SERIOUS BACTERIAL, FUNGAL, VIRAL, OR OPPORTUNISTIC INFECTIONS, INCLUDING TB), MALIGNANCY (INCLUDING NONMELANOMA SKIN CANCER)

Interactions ⬆ ⬇

Drug-drug:

May ↑ risk of bleeding and thrombocytopenia when used with antiplatelet drugs, excluding low-dose aspirin (≤81 mg/day); concurrent use during 1st 3 mo of abrocitinib contraindicated.
Moderate to strong inhibitors of both CYP2C9 and CYP2C19, including fluconazole, significantly ↑ levels and risk of toxicity; avoid concurrent use.
Strong CYP2C9 inducers and strong CYP2C19 inducers, including rifampin, ↓ levels and effectiveness; avoid concurrent use.
Strong CYP2C19 inhibitors, including fluvoxamine, may ↑ levels and risk of toxicity; ↓ abrocitinib dose.
May ↑ levels and risk of toxicity of P-glycoprotein substrates, including dabigatran; closely monitor.
May ↑ risk of adverse reactions and ↓ antibody response to live vaccines; avoid concurrent use.

Route/Dosage ⬆ ⬇

PO (Adults and Children ≥12 yr): 100 mg once daily initially; if adequate response not achieved after 12 wk, may ↑ to 200 mg once daily. Discontinue therapy if inadequate response after dose ↑ to 200 mg once daily. CYP2C19 poor metabolizers or concurrent use of strong CYP2C19 inhibitors: 50 mg once daily initially; if adequate response not achieved after 12 wk, may ↑ to 100 mg once daily. Discontinue therapy if inadequate response after dose ↑ to 100 mg once daily.

Renal Impairment

PO (Adults and Children ≥12 yr): CCr 30–59 mL/min: 50 mg once daily initially; if adequate response not achieved after 12 wk, may ↑ to 100 mg once daily. Discontinue therapy if inadequate response after dose ↑ to 100 mg once daily.

Availability ⬆ ⬇

Tablets: 50 mg; 100 mg; 200 mg

Assessment ⬆ ⬇

Assess involved area of skin before starting and periodically during therapy.
Determine TB infection status. For patients with latent TB or those with a negative latent TB test who are at high risk for TB, start preventive therapy for latent TB before starting abrocitinib. Monitor all patients for active TB during treatment, even patients with initial negative latent TB test.
Conduct viral hepatitis screening in accordance with clinical guidelines. Starting abrocitinib is not recommended in patients with active hepatitis B or hepatitis C.
Monitor for development of signs and symptoms of infection, including TB, during and after therapy. If a serious or opportunistic infection, discontinue therapy. Begin diagnostic testing and antimicrobial therapy. Consider risks and benefits of therapy before reinitiating therapy.
Monitor for signs and symptoms of major adverse cardiac events. Patients who are current or past smokers and patients with other cardiovascular risk factors are at greatest risk.
Monitor for thrombosis, including DVT, PE, and arterial thrombosis. If symptoms of thrombosis occur, discontinue therapy and evaluate and treat patients.

Lab Test Considerations:

Monitor CBC with differential at baseline, 4 wk after starting therapy, and 4 wk after ↑ dose. If platelet count <50,000/mm³, permanently discontinue abrocitinib and follow with CBC until >100,000/mm³. If ALC <500/mm³, temporarily discontinue abrocitinib; may be restarted once ALC returns above this value. If ANC <1000/mm³, temporarily discontinue abrocitinib; may be restarted once ANC returns above this value. If Hgb <8 g/dL, temporarily discontinue abrocitinib; may be restarted once Hgb returns above this value.
- May ↑ lipids. Monitor lipid levels after 4 wk of therapy and periodically thereafter.

Implementation ⬆ ⬇

Complete any necessary immunizations, including herpes zoster vaccinations, in agreement with current immunization guidelines prior to starting therapy.
Can be used with or without topical corticosteroids.
PO: Administer without regard to food, at the same time each day. DNC: Swallow tablets whole with water; do not crush, split, or chew.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take as directed. Take missed dose as soon as possible unless <12 hr before next dose. If <12 hr before next dose, omit dose and resume dosing at the regular scheduled time.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Advise patient to notify health care professional if signs and symptoms of infection (fever, sweating, or chills; blood in phlegm; diarrhea or stomach pain; muscle aches; weight loss; burning during urination or urinating more often than usual; cough or shortness of breath; warm, red, or painful skin or sores on body; feeling very tired) occur.
Caution patients with signs and symptoms of a heart attack or stroke (discomfort in the center of chest that lasts for more than a few minutes or that goes away and comes back; severe tightness, pain, pressure, or heaviness in chest, throat, neck, or jaw; pain or discomfort in arms, back, neck, jaw, or stomach; weakness in one part or on one side of the body; slurred speech; shortness of breath with or without chest discomfort; breaking out in a cold sweat; nausea or vomiting; light-headedness) to notify health care professional immediately.
Inform patient of ↑ risk of DVT and pulmonary embolism. If signs and symptoms (swelling, pain, or tenderness in one or both legs; sudden, unexplained chest or upper back pain; shortness of breath or difficulty breathing) occur, stop therapy and get immediate medical care. Advise patient to notify health care professional if they have had blood clots in the legs or lungs in the past.
May ↑ risk of cancer. Advise patient to have skin checked for skin cancer during therapy. Limit amount of time spent in sunlight. Avoid using tanning beds or sunlamps. Wear protective clothing and use sunscreen with a high protection factor (SPF 30 and above); especially important for patients with very fair skin or with a family history of skin cancer. Instruct patient to notify health care professional if they have ever had any type of cancer.
Rep: Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected. Advise to avoid breastfeeding during and for one day after last dose. May impair female fertility; may be reversible. There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to abrocitinib during pregnancy. Pregnant women exposed to abrocitinib and health care providers are encouraged to call 1-877-311-3770 or visit www.cibinqopregnancyregistry.com.

Evaluation/Desired Outcomes ⬆ ⬇

Improvement in clinical and symptomatic parameters of atopic dermatitis.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

0069- Pfizer Laboratories Div Pfizer Inc
- 0069-0235- Cibinqo
  - 0069-0235-30- 30 TABLET, FILM COATED in 1 BOTTLE (0069-0235-30)

0069- Pfizer Laboratories Div Pfizer Inc
- 0069-0335- Cibinqo
  - 0069-0335-30- 30 TABLET, FILM COATED in 1 BOTTLE (0069-0335-30)

0069- Pfizer Laboratories Div Pfizer Inc
- 0069-0435- Cibinqo
  - 0069-0435-30- 30 TABLET, FILM COATED in 1 BOTTLE (0069-0435-30)

53869- Pfizer Manufacturing Deutschland GmbH
- 53869-1235-
  - 53869-1235-8- 48 BOTTLE in 1 BOX (53869-1235-8) / 30 TABLET, FILM COATED in 1 BOTTLE (53869-1235-1)

53869- Pfizer Manufacturing Deutschland GmbH
- 53869-1235-
  - 53869-1235-9- 48 BOTTLE in 1 BOX (53869-1235-9) / 14 TABLET, FILM COATED in 1 BOTTLE (53869-1235-4)

53869- Pfizer Manufacturing Deutschland GmbH
- 53869-1335-
  - 53869-1335-8- 48 BOTTLE in 1 BOX (53869-1335-8) / 30 TABLET, FILM COATED in 1 BOTTLE (53869-1335-1)

53869- Pfizer Manufacturing Deutschland GmbH
- 53869-1335-
  53869-1335-9- 48 BOTTLE in 1 BOX (53869-1335-9) / 14 TABLET, FILM COATED in 1 BOTTLE (53869-1335-4)

53869- Pfizer Manufacturing Deutschland GmbH
- 53869-1435-
  53869-1435-8- 48 BOTTLE in 1 BOX (53869-1435-8) / 30 TABLET, FILM COATED in 1 BOTTLE (53869-1435-1)

53869- Pfizer Manufacturing Deutschland GmbH
- 53869-1435-
  53869-1435-9- 48 BOTTLE in 1 BOX (53869-1435-9) / 14 TABLET, FILM COATED in 1 BOTTLE (53869-1435-4)

63539- U.S. Pharmaceuticals
- 63539-236- CIBINQO
  63539-236-14- 14 TABLET, FILM COATED in 1 BOTTLE (63539-236-14)

63539- U.S. Pharmaceuticals
- 63539-336- CIBINQO
  - 63539-336-14- 14 TABLET, FILM COATED in 1 BOTTLE (63539-336-14)

63539- U.S. Pharmaceuticals
- 63539-436- CIBINQO
  - 63539-436-14- 14 TABLET, FILM COATED in 1 BOTTLE (63539-436-14)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇