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Generic Name
Ruxolitinib
Brand Names
Jakafi, Opzelura
FDA approval date: November 16, 2011
Classification: Janus Kinase Inhibitor
Form: Cream, Tablet
What is Jakafi (Ruxolitinib)?
Jakafi is a kinase inhibitor indicated for treatment of: intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis in adults.
Approved To Treat
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Related Clinical Trials
A Phase 1b Study of Pelabresib (DAK539) add-on to Stable Dose of Ruxolitinib in Japanese Adult Patients With Myelofibrosis
Summary: This Phase 1b, multicenter, open-label study aims to evaluate the safety, pharmacokinetics (PK), and preliminary efficacy of pelabresib as add-on to ruxolitinib in Japanese patients with myelofibrosis (MF).
Phase I/II Study of Nivolumab in Combination With Ruxolitinib in Relapsed or Refractory Classical Hodgkin Lymphoma
Summary: This is a Phase I/II, multicenter, open-label, dose escalation/dose-expansion study to evaluate the tolerability, safety, and the maximum tolerated dose (MTD) of ruxolitinib when given with fixed dose nivolumab in patients with relapsed or refractory classical Hodgkin lymphoma (cHL).
A Phase 3, Randomized, Open-label, Active-Comparator-Controlled Clinical Study to Evaluate the Safety and Efficacy of Bomedemstat (MK-3543/IMG-7289) Versus Best Available Therapy (BAT) in Participants With Essential Thrombocythemia Who Have an Inadequate Response to or Are Intolerant of Hydroxyurea
Summary: This is a study evaluating the safety and efficacy of bomedemstat (MK-3543) compared with the best available therapy (BAT) in participants with essential thrombocythemia (ET) who have an inadequate response to or are intolerant of hydroxyurea. The primary study hypothesis is that bomedemstat is superior to the best available therapy with respect to durable clinicohematologic response (DCHR).
Related Latest Advances
Brand Information
JAKAFI (ruxolitinib)
1DOSAGE FORMS AND STRENGTHS
JAKAFI:
5 mg tablets - round and white with "INCY" on one side and "5" on the other.
10 mg tablets - round and white with "INCY" on one side and "10" on the other.
15 mg tablets - oval and white with "INCY" on one side and "15" on the other.
20 mg tablets - capsule-shaped and white with "INCY" on one side and "20" on the other.
25 mg tablets - oval and white with "INCY" on one side and "25" on the other.
JAKAFI XR:
11 mg extended-release tablets - round and light pink with “I” on one side and “11” on the other.
22 mg extended-release tablets - round and light yellow with “I” on one side and “22” on the other.
33 mg extended-release tablets - round and pink with “I” on one side and “33” on the other.
44 mg extended-release tablets - round and grey with “I” on one side and “44” on the other.
55 mg extended-release tablets - round and yellow with “I” on one side and “55” on the other.
2CONTRAINDICATIONS
None.
3ADVERSE REACTIONS
The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling:
- Thrombocytopenia, Anemia and Neutropenia
- Risk of Infection
- Symptom Exacerbation Following Interruption or Discontinuation of Treatment
- Non-Melanoma Skin Cancer
- Lipid Elevations
- Major Adverse Cardiovascular Events (MACE)
- Thrombosis
- Secondary Malignancies
3.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The safety of JAKAFI XR has been established from adequate and well-controlled studies of JAKAFI in adult patients with myelofibrosis, polycythemia vera, and adult and pediatric patients with acute and chronic graft-versus-host-disease
Myelofibrosis
The safety of JAKAFI was assessed in 617 patients in 6 clinical studies with a median duration of follow-up of 10.9 months, including 301 patients with MF in 2 Phase 3 studies.
In these 2 Phase 3 studies, patients had a median duration of exposure to JAKAFI of 9.5 months (range: 0.5 to 17 months), with 89% of patients treated for more than 6 months and 25% treated for more than 12 months. One hundred and eleven (111) patients started treatment at 15 mg twice daily and 190 patients started at 20 mg twice daily. In patients starting treatment with 15 mg twice daily (pretreatment platelet counts of 100 to 200 × 10
In a double-blind, randomized, placebo-controlled study of JAKAFI, among the 155 patients treated with JAKAFI, the most frequent adverse reactions were thrombocytopenia and anemia
Discontinuation for adverse events, regardless of causality, was observed in 11% of patients treated with JAKAFI and 11% of patients treated with placebo.
Table 15 presents the most common nonhematologic adverse reactions occurring in patients who received JAKAFI in the double-blind, placebo-controlled study during randomized treatment.
Description of Selected Adverse Reactions
Anemia
In the 2 Phase 3 clinical studies, median time to onset of first CTCAE Grade 2 or higher anemia was approximately 6 weeks. One patient (< 1%) discontinued treatment because of anemia. In patients receiving JAKAFI, mean decreases in hemoglobin reached a nadir of approximately 1.5 to 2 g/dL below baseline after 8 to 12 weeks of therapy and then gradually recovered to reach a new steady state that was approximately 1 g/dL below baseline. This pattern was observed in patients regardless of whether they had received transfusions during therapy.
In the randomized, placebo-controlled study, 60% of patients treated with JAKAFI and 38% of patients receiving placebo received red blood cell transfusions during randomized treatment. Among transfused patients, the median number of units transfused per month was 1.2 in patients treated with JAKAFI and 1.7 in placebo treated patients.
Thrombocytopenia
In the 2 Phase 3 clinical studies, in patients who developed Grade 3 or 4 thrombocytopenia, the median time to onset was approximately 8 weeks. Thrombocytopenia was generally reversible with dose reduction or dose interruption. The median time to recovery of platelet counts above 50 x 10
Neutropenia
In the 2 Phase 3 clinical studies, 1% of patients reduced or stopped JAKAFI because of neutropenia.
Table 16 provides the frequency and severity of clinical hematology abnormalities reported for patients receiving treatment with JAKAFI or placebo in the placebo-controlled study.
Additional Data From the Placebo-Controlled Study
- 25% of patients treated with JAKAFI and 7% of patients treated with placebo developed newly occurring or worsening Grade 1 abnormalities in alanine transaminase (ALT). The incidence of greater than or equal to Grade 2 elevations was 2% for JAKAFI with 1% Grade 3 and no Grade 4 ALT elevations.
- 17% of patients treated with JAKAFI and 6% of patients treated with placebo developed newly occurring or worsening Grade 1 abnormalities in aspartate transaminase (AST). The incidence of Grade 2 AST elevations was < 1% for JAKAFI with no Grade 3 or 4 AST elevations.
- 17% of patients treated with JAKAFI and < 1% of patients treated with placebo developed newly occurring or worsening Grade 1 elevations in cholesterol. The incidence of Grade 2 cholesterol elevations was < 1% for JAKAFI with no Grade 3 or 4 cholesterol elevations.
Polycythemia Vera
In a randomized, open-label, active-controlled study, 110 patients with PV resistant to or intolerant of hydroxyurea received JAKAFI and 111 patients received best available therapy (BAT)
Clinically relevant laboratory abnormalities are shown in Table 18.
Acute Graft-Versus-Host Disease
In a single-arm, open-label study, 71 adults (ages 18-73 years) were treated with JAKAFI for aGVHD failing treatment with steroids with or without other immunosuppressive drugs
There were no fatal adverse reactions to JAKAFI. An adverse reaction resulting in treatment discontinuation occurred in 31% of patients. The most common adverse reaction leading to treatment discontinuation was infection (10%). Table 19 shows the adverse reactions other than laboratory abnormalities.
Selected laboratory abnormalities during treatment with JAKAFI are shown in Table 20.
Chronic Graft-Versus-Host Disease
In a Phase 3, randomized, open-label, multi-center study, 165 patients were treated with JAKAFI and 158 patients were treated with BAT for cGVHD failing treatment with steroids with or without other immunosuppressive drugs
There were 5 fatal adverse reactions to JAKAFI, including 1 from toxic epidermal necrolysis and 4 from neutropenia, anemia and/or thrombocytopenia. An adverse reaction resulting in treatment discontinuation occurred in 18% of patients treated with JAKAFI. An adverse reaction resulting in dose modification occurred in 27%, and an adverse reaction resulting in treatment interruption occurred in 23%. The most common hematologic adverse reactions (incidence > 35%) are anemia and thrombocytopenia. The most common nonhematologic adverse reactions (incidence ≥ 20%) are infections (pathogen not specified) and viral infection.
Table 21 presents the most frequent nonlaboratory adverse reactions occurring up to Cycle 7 Day 1 of randomized treatment.
Clinically relevant laboratory abnormalities are shown in Table 22.
3.2Postmarketing Experience
The following adverse reactions have been identified during post-approval use of JAKAFI. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure:
- Infections and Infestations: herpes simplex virus reactivation and/or dissemination
- Metabolism and Nutrition disorders: hypoglycemia
4OVERDOSAGE
There is no known antidote for overdoses with JAKAFI/JAKAFI XR. Single doses up to 200 mg have been given with acceptable acute tolerability. Higher than recommended repeat doses are associated with increased myelosuppression including leukopenia, anemia, and thrombocytopenia. Appropriate supportive treatment should be given.
Hemodialysis is not expected to enhance the elimination of JAKAFI/JAKAFI XR.
5DESCRIPTION
Ruxolitinib phosphate is a kinase inhibitor with the chemical name (
Ruxolitinib phosphate is a white to off-white to light pink powder and is soluble in aqueous buffers across a pH range of 1 to 8.
JAKAFI (ruxolitinib) tablets are for oral administration. Each tablet contains 5 mg, 10 mg, 15 mg, 20 mg, or 25 mg of ruxolitinib free base, equivalent to 6.6 mg, 13.2 mg, 19.8 mg, 26.4 mg, or 33 mg of ruxolitinib phosphate, respectively, and the following inactive ingredients: colloidal silicon dioxide, hydroxypropyl cellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone and sodium starch glycolate.
JAKAFI XR (ruxolitinib) extended-release tablets are for oral administration. Each tablet contains 11 mg, 22 mg, 33 mg, 44 mg, or 55 mg of ruxolitinib free base equivalent to 14.5 mg, 29 mg, 43.6 mg, 58.1 mg, or 72.6 mg of ruxolitinib phosphate, respectively, and the following inactive ingredients: colloidal silicon dioxide, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium stearyl fumarate. In addition, the film coating contains the following inactive ingredients: colorants (black iron oxide, red iron oxide, and yellow iron oxide), copovidone, hypromellose, polydextrose, polyethylene glycol, titanium dioxide, and triglycerides.
6HOW SUPPLIED/STORAGE AND HANDLING
JAKAFI (ruxolitinib) tablets are available as follows:
JAKAFI XR (ruxolitinib) extended-release tablets are available as follows:
Store JAKAFI/JAKAFI XR at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) [see USP Controlled Room Temperature].
Dispense in a tight container. Protect from light.
7PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Patient Information).
Thrombocytopenia, Anemia and Neutropenia
Inform patients that JAKAFI/JAKAFI XR is associated with thrombocytopenia, anemia and neutropenia, and of the need to monitor CBC before and during treatment. Advise patients to observe for and report bleeding
Infections
Inform patients of the signs and symptoms of infection and to report any such signs and symptoms promptly.
Inform patients regarding the early signs and symptoms of herpes zoster and of PML, and advise patients to seek the advice of a clinician if such symptoms are observed
Symptom Exacerbation Following Interruption or Discontinuation of Treatment
Inform patients that after discontinuation of treatment, signs and symptoms from myeloproliferative neoplasms may flare. Instruct patients not to interrupt or discontinue JAKAFI/JAKAFI XR therapy without consulting their healthcare provider
Non-Melanoma Skin Cancer
Inform patients that JAKAFI/JAKAFI XR may increase their risk of certain NMSCs. Advise patients to inform their healthcare provider if they have ever had any type of skin cancer or if they observe any new or changing skin lesions
Lipid Elevations
Inform patients that JAKAFI/JAKAFI XR may increase blood cholesterol, and of the need to monitor blood cholesterol levels
Major Adverse Cardiovascular Events
Advise patients that events of MACE including myocardial infarction, stroke, and cardiovascular death, have been reported in clinical studies with another JAK-inhibitor used to treat rheumatoid arthritis, a condition for which JAKAFI/JAKAFI XR is not indicated. Advise patients, especially current or past smokers or patients with other cardiovascular risk factors, to be alert for the development of signs and symptoms of cardiovascular events
Thrombosis
Advise patients that events of DVT and PE have been reported in clinical studies with another JAK-inhibitor used to treat rheumatoid arthritis, a condition for which JAKAFI/JAKAFI XR is not indicated. Advise patients to tell their healthcare provider if they develop any signs or symptoms of a DVT or PE
Secondary Malignancies
Advise patients, especially current or past smokers and patients with a known secondary malignancy (other than a successfully treated NMSC), that lymphoma and other malignancies (excluding NMSC) have been reported in clinical studies with another JAK-inhibitor used to treat rheumatoid arthritis, a condition for which JAKAFI/JAKAFI XR is not indicated
Drug-Drug Interactions
Advise patients to inform their healthcare providers of all medications they are taking, including over-the-counter medications, herbal products and dietary supplements
Dialysis
Inform patients on dialysis that their dose should not be taken before dialysis but only following dialysis
Lactation
Inform women not to breastfeed during treatment with JAKAFI/JAKAFI XR and for 2 weeks after the final dose
Compliance
Advise patients to continue taking JAKAFI/JAKAFI XR every day for as long as their physician tells them and that this is a long-term treatment. Patients should not change dose or stop taking JAKAFI/JAKAFI XR without first consulting their physician. Patients should be aware that after discontinuation of treatment, signs and symptoms from myeloproliferative neoplasms are expected to return.
Manufactured for:
JAKAFI is a registered trademark of Incyte.
8mg Tablet Bottle Label
Rx only
NDC 50881-005-60
Jakafi® (Ruxolitinib) Tablets
5 mg
60 tablets
Each tablet contains 6.6 mg ruxolitinib phosphate equivalent to 5 mg ruxolitinib free base.
9mg Tablet Bottle Label
Rx only
NDC 50881-010-60
Jakafi® (Ruxolitinib) Tablets
10 mg
60 tablets
Each tablet contains 13.2 mg ruxolitinib phosphate equivalent to 10 mg ruxolitinib free base.
10mg Tablet Bottle Label
Rx only
NDC 50881-015-60
Jakafi® (Ruxolitinib) Tablets
15 mg
60 tablets
Each tablet contains 19.8 mg ruxolitinib phosphate equivalent to 15 mg ruxolitinib free base.
11mg Tablet Bottle Label
Rx only
NDC 50881-020-60
Jakafi® (Ruxolitinib) Tablets
20 mg
60 tablets
Each tablet contains 26.4 mg ruxolitinib phosphate equivalent to 20 mg ruxolitinib free base.
12mg Tablet Bottle Label
Rx only
NDC 50881-025-60
Jakafi® (Ruxolitinib) Tablets
25 mg
60 tablets
Each tablet contains 33 mg ruxolitinib phosphate equivalent to 25 mg ruxolitinib free base.
13mg Tablet Bottle Label
Rx only
NDC 50881-011-08
Jakafi XR™ (ruxolitinib) extended-release tablets
11 mg
30 tablets
Each tablet contains 14.5 mg ruxolitinib phosphate equivalent to 11 mg ruxolitinib free base.
14mg Tablet Bottle Label
Rx only
NDC 50881-022-08
Jakafi XR™ (ruxolitinib) extended-release tablets
22 mg
30 tablets
Each tablet contains 29 mg ruxolitinib phosphate equivalent to 22 mg ruxolitinib free base.
15mg Tablet Bottle Label
Rx only
NDC 50881-033-08
Jakafi XR™ (ruxolitinib) extended-release tablets
33 mg
30 tablets
Each tablet contains 43.6 mg ruxolitinib phosphate equivalent to 33 mg ruxolitinib free base.
16mg Tablet Bottle Label
Rx only
NDC 50881-044-08
Jakafi XR™ (ruxolitinib) extended-release tablets
44 mg
30 tablets
Each tablet contains 58.1 mg ruxolitinib phosphate equivalent to 44 mg ruxolitinib free base.
17mg Tablet Bottle Label
Rx only
NDC 50881-055-08
Jakafi XR™ (ruxolitinib) extended-release tablets
55 mg
30 tablets
Each tablet contains 72.6 mg ruxolitinib phosphate equivalent to 55 mg ruxolitinib free base.
