Abrocitinib side effects

Generic Name: Abrocitinib
Brand name: Cibinqo

Medically reviewed by A Ras MD.  Last updated March 25, 2022

What is Abrocitinib 

Abrocitinib side effects Are the unwanted reactions that may be experienced while using Abrocitinib.

Abrocitinib can be prescribed that acts as a Janus Kinase (JAK) inhibitor. Abrocitinib is prescribed for adults suffering from moderate to severe Atopic skin eczema (eczema) that does not respond to treatments and cannot be managed with prescription treatments which include biologic medicines, or in adults who can’t take these treatments.

Abrocitinib is a white to pale colored powder with the following chemical name: N-((1s,3s)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide

The solubility of abrocitinib in water is 0.04 mg/mL at 25ºC.

Abrocitinib has a molecular weight of 323.42 g/mol and a molecular formula of C14H21N5O2S. The structural formula of abrocitinib is:

Cibinqo

Each film-coated tablet contains 50 mg or 100 mg or 200 mg of abrocitinib and the following inactive ingredients: dibasic calcium phosphate anhydrous, hypromellose, iron oxide red, lactose monohydrate, Macrogol, magnesium stearate, microcrystalline cellulose, sodium starch glycolate, titanium dioxide, and triacetin.

It isn’t known whether Abrocitinib is safe and effective for children.

In the initial 3 months of your treatment use Abrocitinib. Do not combine Abrocitinib alongside other medications that stop blood clots. Aspirin can be taken in low doses up to 81 mg daily during this time if recommended by your physician.

Boxed Warnings

WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, AND THROMBOSIS

Serious Infections

Patients treated with Abrocitinib may be at increased risk for developing serious infections that may lead to hospitalization or death; The most frequent serious infections reported with Abrocitinib were herpes simplex, herpes zoster, and pneumonia.

If a serious or opportunistic infection develops, discontinue Abrocitinib and control the infection.

Reported infections from Janus kinase (JAK) inhibitors used to treat inflammatory conditions:

  • Active tuberculosis 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 the use of Abrocitinib in patients with an active, serious infection including localized infections. The risks and benefits of treatment with Abrocitinib should be carefully considered prior to initiating therapy in patients with chronic or recurrent infections.

Patients should be closely monitored for the development of signs and symptoms of infection during and after treatment with Abrocitinib, including the possible development of tuberculosis in patients who tested negative for latent tuberculosis infection prior to initiating therapy

Mortality

In a large, randomized, postmarketing safety study in rheumatoid arthritis (RA) patients 50 years of age and older with at least one cardiovascular risk factor comparing another JAK inhibitor to TNF blocker treatment, a higher rate of all-cause mortality, including sudden cardiovascular death, was observed with the JAK inhibitor. Abrocitinib is not approved for use in RA patients.

Malignancies

Malignancies were reported in patients treated with Abrocitinib. Lymphoma and other malignancies have been observed in patients receiving JAK inhibitors used to treat inflammatory conditions. In RA patients treated with another JAK inhibitor, a higher rate of malignancies (excluding non-melanoma skin cancer (NMSC)) was observed when compared with TNF blockers. Patients who are current or past smokers are at additional increased risk.

Major Adverse Cardiovascular Events

Major adverse cardiovascular events were reported in patients treated with Abrocitinib. In RA patients 50 years of age and older with at least one cardiovascular risk factor treated with another JAK inhibitor, a higher rate of major adverse cardiovascular events (MACE) (defined as cardiovascular death, myocardial infarction, and stroke), was observed when compared with TNF blockers. Patients who are current or past smokers are at additional increased risk. Discontinue Abrocitinib in patients that have experienced a myocardial infarction or stroke.

Thrombosis

Deep venous thrombosis (DVT) and pulmonary embolism (PE) have been reported in patients treated with Abrocitinib. Thrombosis, including PE, DVT, and arterial thrombosis have been reported in patients receiving JAK inhibitors used to treat inflammatory conditions. Many of these adverse reactions were serious and some resulted in death. In RA patients 50 years of age and older with at least one cardiovascular risk factor treated with another JAK inhibitor, a higher rate of thrombosis was observed when compared with TNF blockers. Avoid Abrocitinibin patients at risk. If symptoms of thrombosis occur, discontinue Abrocitinib and treat appropriately.

Variations in certain laboratory test results

Your doctor should conduct blood tests prior to you beginning taking this medication  and throughout the treatment using this medication to determine the following:

  • A low number of lymphocytes. The lymphocytes contain white blood cells that aid your body fight infections.
  • low neutrophil count. Neutrophils are blood-forming white cells that help the body fight off infections.
  • Low red blood cell count. This could mean you are suffering from anemia. This can cause you to feel tired and weak.
  • Low platelet count. Platelets aid in the formation of clots and stop bleeding or stop it.

It is not recommended to consume Abrocitinib in the event that your lymphocyte count or neutrophil counts, the number of red blood cells as well as platelet counts, are low. Your doctor may decide to suspend you from taking Abrocitinib therapy for a short period of time in the event of changes in the results of these blood tests. You could also experience changes in other tests, for instance, the cholesterol levels in your blood.

Your healthcare professional should perform blood tests around 4 weeks after starting taking Abrocitinib and four weeks following any increase in the dosage of Abrocitinib to determine the blood cell count and the frequency required for other tests at the lab.

What Abrocitinib side effects

The most frequent adverse effects of Abrocitinib are:

Read “What do you think is the most significant thing I should be aware of about Abrocitinib.

  • common cold
  • vomiting
  • nausea
  • Tongue and throat pain
  • headache
  • Flu
  • herpes simplex including
  • stomach sores from the cold flu
  • bacterial skin infection (impetigo)
  • Increased blood sugar
  • Creatinine levels in high blood pressure
  • an allergic skin rash that is caused by the substance you were in contact with
  • dizziness
  • Pain in the stomach area
  • Urinary tract infection
  • Shingles
  • tiredness
  • Low platelet count
  • Acne

Abrocitinib could cause fertility issues in females. This could limit your ability to become pregnant. Discuss with your physician should you have any concerns regarding fertility.

The tear or separation of the inner lining of the back of the eyes (retinal detachment) is a common occurrence in patients suffering from atopic dermatitis and which is treated by Abrocitinib. Consult your healthcare professional right now if you notice abrupt changes in your vision after treatments with Abrocitinib.

These are not the only possible side effects associated with Abrocitinib.

Experiences in Clinical Trials

Since studies conducted in clinical trials happen in diverse conditions, the rate of adverse reactions that are observed in trials for a particular drug can’t be directly compared with rates observed in clinical trials for another drug, and they may not be reflected in the actual rates in.

The safety of Abrocitinib was assessed in four placebo-controlled, randomized trial studies (2 monotherapy, one combination therapy using corticosteroid applied to the skin, and one dose-ranging) and one extended-term study in patients with moderate to severe Atopic skin atopic dermatitis (AD). The total number of people who suffered from moderate to severe skin conditions were treated with Abrocitinib during these trials, representing 1428 patient-years of exposure. There were 634 subjects who had at least one year of experience with Abrocitinib.

In the clinical trials that were placebo-controlled, eleven98 subjects had been exposed Abrocitinib 608 of them received Abrocitinib 100 mg once a day, and 590 people got Abrocitinib 200 mg every day for up to 16 weeks. The average age of the subject was 33.0 years. 124 of the subjects (8.1 percent) were aged 12 to not more than age 18, and more than 94 (6.1 percent) were old or older. The majority of the subjects were White (68.7 percent) as well as male (53.9 53.9 %). Although subjects aged between 12 and 17 years of age were involved in the trials, Abrocitinib is not approved to be used in children.

Acute reactions that exceed 1 percent in any of the treatment groups and more frequently than that of the group with no treatment are reported in Table. There were 61 (5.1 percent) patients that were treated with Abrocitinib were removed from the study because of adverse reactions. The safety assessment that was observed for Abrocitinib for monotherapy, as well as those in combination trial(s), were comparable.

 

Table. Negative Reactions to Placebo-Controlled Clinical Trials reported in more than 1 percent of CIBINQO treated subjects with moderate to severe atopic Dermatitis, and at a Higher Ratio Than Placebo in up to 16 weeks.

Weeks 0–16
CIBINQO
200 mg
N=590
n (%*)
CIBINQO
100 mg
N=608
n (%*)
Placebo
N=342
n (%*)
Nasopharyngitis 51 (8.7) 75 (12.4) 27 (7.9)
Nausea 86 (14.5) 37 (6.0) 7 (2.1)
Headache 46 (7.8) 36 (6.0) 12 (3.5)
Herpes simplex 25 (4.2) 20 (3.3) 6 (1.8)
Increased blood creatinine phosphokinase 17 (2.9) 14 (2.3) 5 (1.5)
Dizziness 17 (2.9) 11 (1.8) 3 (0.9)
Urinary tract infection 13 (2.2) 10 (1.7) 4 (1.2)
Fatigue 8 (1.3) 10 (1.6) 2 (0.5)
Acne 28 (4.7) 10 (1.6) 0 (0.0)
Vomiting 19 (3.2) 9 (1.5) 3 (0.9)
Impetigo 3 (0.5) 9 (1.5) 1 (0.3)
Oropharyngeal pain 6 (1.0) 8 (1.4) 2 (0.6)
Hypertension 5 (0.8) 7 (1.2) 2 (0.7)
Influenza 6 (1.1) 7 (1.2) 0 (0.0)
Gastroenteritis 8 (1.3) 7 (1.1) 2 (0.6)
Dermatitis contact 3 (0.5) 6 (1.1) 1 (0.3)
Abdominal pain upper 11 (1.9) 4 (0.6) 0 (0.0)
Abdominal discomfort 7 (1.2) 3 (0.5) 1 (0.3)
Herpes zoster 7 (1.2) 2 (0.3) 0 (0.0)
Thrombocytopenia 9 (1.5) 0 (0.0) 0 (0.0)

*Study size adjusted percentages

†Herpes simplex also includes oral herpes, ophthalmic herpes, herpes dermatitis, genital herpes.

Specific adverse reactions

Exposure-adjusted incidence rates were adjusted based on the trial size for all adverse reactions that were reported in this section.

All-Over Infections

In the placebo-controlled studies, over a period of up to sixteen weeks, total infections were observed within 90 patients (126.8 percent of 100 year-olds) that were given a placebo, 211 patients (168.8 per 100 years of patient-years) who were treated using Abrocitinib 100 mg, and the 204 subjects (159.5 per 100 patient-years) who were treated with Abrocitinib 200 mg. In all five clinical trials, which included the extended-term trial all infections were recorded in 427 patients (91.8 per 100 patient-years) who were treated by Abrocitinib 100 mg, and 394 patients (103.2 per 100 patient-years) who were treated by Abrocitinib 200 mg.

More serious infections

In the placebo-controlled trials lasting up to 16 weeks, severe infections were detected in two patients (2.6 for 100 years of patient care) who were treated using a placebo. six patients (3.9 per 100 years of patient-years) were treated using Abrocitinib 100 mg. There were also two subjects (1.3 for 100 years of patient care) that were given Abrocitinib 200 mg. In all five clinical trials, which included the long-term extension trial serious infections were observed in 18 patients (2.3 per 100 years of patient-years) who have been treated with Abrocitinib100 mg, and sixteen subjects (2.3 per 100 years of patient-years) who were treated by Abrocitinib 200 mg. The most frequently diagnosed serious illnesses were herpes simplex herpes zoster, as well as pneumonia.

Herpes Zoster

In the placebo-controlled clinical trials lasting up to 16 weeks, the opportunistic infections were typically multidermatomal cutaneous herpes Zoster. Herpes zoster was observed in 0 people treated with placebo, three patients (1.9 per 100 patient-years) that were given Abrocitinib 100 mg, and eight subjects (5.1 per 100 patient-years) that were given Abrocitinib 200 mg. In all five clinical trials, including the lengthy extension trial, Herpes zoster was found in 16 patients (2.0 per 100 patient-years) that were given Abrocitinib 100 mg, and in 35 patients (5.2 per 100 patient-years) who were treated using Abrocitinib 200 mg.

Malignancy

In the placebo-controlled trials lasting up to 16 weeks, there was no malignancy was observed in patients who received either placebo and Abrocitinib 100 mg, and in one person (0.65 per 100 patient-years) who was treated by Abrocitinib 200 mg. In all five clinical trials, which included the extended-term trial the malignancy was found in four participants (0.5 per 100 patient-years) who were treated by Abrocitinib100 mg, and in two patients (0.3 per 100 years of patient-years) who were treated by Abrocitinib 200 mg.

Thrombosis

In the clinical trials in all of them, including the extended-term trial, there was a report of pulmonary embolism in 3 patients (0.4 per 100 patient-years) that were treated with 200 mg Abrocitinib. Deep vein thrombosis has been reported in two patients (0.3 per 100 patient-years) that were treated with Abrocitinib 200 mg. The thrombosis was not present when subjects were who were treated using Abrocitinib 100 mg.

Major adverse Cardiovascular Events

In the placebo-controlled studies, during up to 16 weeks major adverse cardiovascular events (MACE) were recorded in 1 patient (0.6 per 100 years of patient-years) that was treated using Abrocitinib 100 mg. In all five clinical trials, including the lengthy extension trial, MACE was observed in one person (0.1 per 100 years of patient-years) who was treated by Abrocitinib 100 mg, and in two patients (0.3 per 100 patient-years) that were treated using Abrocitinib 200 mg.

Thrombocytopenia

In the placebo-controlled clinical trials for up to 16 weeks treatment with Abrocitinib was linked to a dose-related reduction in the number of platelets. The most significant effects on platelets were seen after 4 weeks after which it returned to the baseline level despite continuing treatment. In all five clinical trials, which included the extended-term trial, 6 patients (0.9 per 100 patient-years) were treated with Abrocitinib 200 mg suffered adverse reactions to thrombocytopenia. none of the subjects who received Abrocitinib 100 mg experienced an adverse reaction related to thrombocytopenia.

Lymphopenia

In the placebo-controlled studies which ran up to 16 weeks, the confirmation of ALC of 500/mm3 was observed in 2 patients (1.2 per 100 years of patient-years) who were treated using Abrocitinib 200 mg and zero subjects that were treated by Abrocitinib 100 mg and placebo. Both cases occurred during the initial 4 weeks after exposure.

Lipid Elevations

In the placebo-controlled tests during up to 16 weeks, it was observed that there was a dose-dependent increase in the levels of low-density lipoprotein cholesterol (LDL-c) as well as total cholesterol and high-density lipoprotein cholesterol (HDL-c) as compared to placebo at Week 4, that remained elevated until the last visit of the period of treatment. The adverse reactions associated with hyperlipidemia were observed in one subject (0.6 per 100 patient-years) who have exposed to Abrocitinib100 mg, three individuals (2.0 per 100 patient-years) who have exposed to Abrocitinib 200 mg.

Retinal Detachment

In the placebo-controlled studies, during up to 16 weeks retinal detachment was seen in just one patient (0.6 per 100 years of patient-years) who received Abrocitinib100 mg. In all five clinical trials, which included the extension trial for long-term duration retinal detachment was observed in two patients (0.3 per 100 years of patient-years) who were treated using Abrocitinib100 mg.

Creatine Phosphokinase Elevations (CPK)

In the placebo-controlled trial for up to 16 weeks, signs of blood CPK elevated were noted in six patients (7.5 per 100 patient-years) who were treated with placebo. eleven subjects (6.9 per 100 years of patient-years) receiving 100 mg Abrocitinib as well as 19 patients (12.3 per 100 years of patient-years) receiving 200 mg Abrocitinib. The majority of elevations were transient, there were no reports of adverse reactions to rhabdomyolysis.

General information on the safety of Abrocitinib.

Some medicines are prescribed for reasons that are not the ones listed in the Medication Guide. Don’t use Abrocitinib to treat a condition for that it is not recommended. Do not give Abrocitinib to other people, even though they suffer from the same symptoms that you do. It could cause harm to them.

Label

PRINCIPAL DISPLAY PANEL – 50 MG TABLET BOTTLE LABEL

  • ALWAYS DISPENSE WITH
    MEDICATION GUIDE
  • Pfizer
    NDC 0069-0235-30
  • CIBINQO
    (abrocitinib) tablets
  • 50 mg
  • Do not crush, split, or chew the tablets.
  • 30 Tablets
    Rx only
Cibinqo

PRINCIPAL DISPLAY PANEL – 100 MG TABLET BOTTLE LABEL

  • ALWAYS DISPENSE WITH
    MEDICATION GUIDE
  • Pfizer
    NDC 0069-0335-30
  • CIBINQO
    (abrocitinib) tablets
  • 100 mg
  • Do not crush, split, or chew the tablets.
  • 30 Tablets
    Rx only

 

Cibinqo

 

PRINCIPAL DISPLAY PANEL – 200 MG TABLET BOTTLE LABEL

  • ALWAYS DISPENSE WITH
    MEDICATION GUIDE
  • Pfizer
    NDC 0069-0435-30
  • CIBINQO
    (abrocitinib) tablets
  • 200 mg
  • Do not crush, split, or chew the tablets.
  • 30 Tablets
    Rx only

 

Abrocitinib side effects

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