Ruxolitinib phosphate

What is Ruxolitinib phosphate?

Ruxolitinib phosphate (Jakafi) is a kinase inhibitor used to treat:

• myelofibrosis (MF)
• polycythemia vera
• acute graft-versus-host-disease (aGVHD) who have taken corticosteroids
• chronic graft-versus-host-disease (cGVHD)

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Ruxolitinib Structural formula V1

Ruxolitinib2DACS

What are the uses of this medicine?

Ruxolitinib phosphate (Jakafi) is used to treat:

• adults with certain types of myelofibrosis (MF).
• adults with polycythemia vera (PV) who have already taken a medicine called hydroxyurea and it did not work well enough or they could not tolerate it.
• adults and children 12 years of age and older with acute graft-versus-host-disease (aGVHD) who have taken corticosteroids and they did not work well enough.
• adults and children 12 years of age and older with chronic graft-versus-host-disease (cGVHD) who have taken one or two types of treatments and they did not work well enough.

How does this medicine work?

• The phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.
• Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation.
• The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications listed above and any of the following:

• antifungal medications including itraconazole (Sporanox), ketoconazole, and voriconazole (Vfend)
• carbamazepine (Carbatrol, Equetro, Tegretol, others)
• clarithromycin
• efavirenz (Sustiva, in Atripla, Symfi)
• erythromycin (E.E.S, Eryc, Ery-tab)
• fluconazole (Diflucan)
• HIV protease inhibitors including indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir, in Kaletra, Viekira Pak), and saquinavir (Invirase)
• nefazodone
• nevirapine (Viramune)
• phenytoin (Dilantin, Phenytek)
• pioglitazone (Actos, in Oseni, Duetact)
• rifabutin (Mycobutin)
• rifampin (Rifadin, Rimactane, in Rifamate, Rifater)
• telaprevir (Incivik)
• St. John's wort

Is this medicine FDA approved?

• In November 2011, ruxolitinib was approved by the U.S. Food and Drug Administration (FDA) for the treatment of intermediate or high-risk myelofibrosis.
• In 2014, it was approved in polycythemia vera (PCV) when there has been an inadequate response to or intolerance of hydroxyurea.

How should this medicine be used?

Recommended dosage: Myelofibrosis: The starting dose of Jakafi is based on patient’s baseline platelet count:

• Greater than 200 x 109/L: 20 mg given orally twice daily
• 100 x 109/L to 200 x 109/L: 15 mg given orally twice daily
• 50 x 109/L to less than 100 x 109/L: 5 mg given orally twice daily

• Monitor complete blood counts every 2 to 4 weeks until doses are stabilized, and then as clinically indicated.
• Modify or interrupt dosing for thrombocytopenia.

Polycythemia Vera:

• The starting dose of Jakafi is 10 mg given orally twice daily.

Acute Graft-Versus-Host Disease:

• The starting dose of Jakafi is 5 mg given orally twice daily.

Chronic Graft-Versus-Host Disease:

• The starting dose of Jakafi is 10 mg given orally twice daily.

Administration:

• You can take Jakafi with or without food.
• Jakafi may also be given through certain nasogastric tubes.
• If you miss a dose of Jakafi, take your next dose at your regular time. Do not take 2 doses at the same time.
• You will have regular blood tests during your treatment with Jakafi. Your healthcare provider may change your dose of Jakafi or stop your treatment based on the results of your blood tests.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 5 mg, 10 mg, 15 mg, 20 mg and 25 mg.

This medicine is available in fallowing brand namesː

• Jakafi

What side effects can this medication cause?

The most common side effects of Jakafi in adults with certain types of myelofibrosis (MF) and polycythemia vera include:

• low platelet counts
• low red blood cell counts
• bruising
• dizziness
• headache
• diarrhea

The most common side effects of Jakafi in people with acute graft-versus-host-disease (aGVHD) include:

• low red blood cell counts
• low platelet counts
• low white blood cell counts
• infections
• swelling

The most common side effects of Jakafi in people with chronic graft-versus-host-disease (cGVHD) include:

• low red blood cell counts
• low platelet counts
• infections, including viral infections

Jakafi can cause serious side effects including:

• Low blood cell counts
• Infection
• Cancer
• Cholesterol increases
• Increased risk of
• blood clots
• Possible increased risk of new (secondary) cancers

What special precautions should I follow?

• Treatment with Jakafi can cause thrombocytopenia, anemia and neutropenia. Manage by dose reduction, or interruption, or transfusion.
• Serious bacterial, mycobacterial, fungal and viral infections have occurred. Assess patients for signs and symptoms of infection and initiate appropriate treatment promptly. Serious infections should have resolved before starting therapy with Jakafi.
• Following discontinuation of Jakafi, symptoms from myeloproliferative neoplasms may return to pretreatment levels over a period of approximately one week. Manage with supportive care and consider resuming treatment with Jakafi.
• Non-melanoma skin cancers including basal cell, squamous cell, and Merkel cell carcinoma have occurred in patients treated with Jakafi. Perform periodic skin examinations.
• Treatment with Jakafi has been associated with increases in lipid parameters including total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides. Assess lipid levels 8-12 weeks from start of therapy and treat as needed.
• Another JAK-inhibitor has increased the risk of MACE, including cardiovascular death, myocardial infarction, and stroke (compared to those treated with TNF blockers) in patients with rheumatoid arthritis, a condition for which Jakafi is not indicated. Monitor for development of MACE.
• Another JAK-inhibitor has increased the risk of thrombosis, including deep venous thrombosis (DVT), pulmonary embolism (PE), and arterial thrombosis (compared to those treated with TNF blockers) in patients with rheumatoid arthritis, a condition for which Jakafi is not indicated. Evaluate and treat symptoms of thrombosis promptly.
• Monitor for development of secondary malignancies, particularly in patients who are current or past smokers.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• myelosuppression including leukopenia
• anemia
• thrombocytopenia

Management of overdosage:

• Appropriate supportive treatment should be given.
• Hemodialysis is not expected to enhance the elimination of Jakafi.

Can this medicine be used in pregnancy?

• It is not known if Jakafi will harm your unborn baby.

Can this medicine be used in children?

• It is not known if Jakafi is safe or effective in children for treatment of myelofibrosis or polycythemia vera.

What are the active and inactive ingredients in this medicine?

• Active ingredient: ruxolitinib phosphate
• Inactive ingredients: microcrystalline cellulose, lactose monohydrate, magnesium stearate, colloidal silicon dioxide, sodium starch glycolate, povidone and hydroxypropyl cellulose

Who manufactures and distributes this medicine?

Manufactured for:

• Incyte Corporation, 1801 Augustine Cut-off, Wilmington, DE
• Jakafi is a registered trademark of Incyte.

What should I know about storage and disposal of this medication?

• Store Jakafi at room temperature 68°F to 77°F (20°C to 25°C).

• Dailymed label info on Ruxolitinib phosphate
• FDA Ruxolitinib phosphate

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