Pacritinib

What is Pacritinib?

• Pacritinib (Vonjo) is a kinase inhibitor used to treat intermediate or high-risk primary or secondary (post-polycythemia vera or post-essential thrombocythemia) myelofibrosis in adults with low platelets.

Pacritinib skeletal

What are the uses of this medicine?

• Pacritinib (Vonjo) is a prescription medicine used to treat adults with certain types of myelofibrosis who have a platelet count below 50 x 109/L.

How does this medicine work?

• An orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity.
• Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis.
• JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders; the JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617.
• The JAK-STAT signaling pathway is a major mediator of cytokine activity.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• using strong CYP3A4 inhibitors or inducers.

What drug interactions can this medicine cause?

• Avoid use with moderate CYP3A4 inhibitors or inducers.
• Coadministration of Vonjo can alter the concentration of drugs that are P-gp, BCRP, or OCT1 substrates. Avoid use with sensitive substrates.

Is this medicine FDA approved?

• Vonjo was approved for medical use in the United States in February 2022.

How should this medicine be used?

Recommended dosage:

• The recommended dosage of Vonjo is 200 mg orally twice daily. Vonjo may be taken with or without food.

Administration:

• Take Vonjo exactly as your healthcare provider tells you to take it.
• Do not change your dose or stop taking Vonjo without first talking to your healthcare provider.
• If you take other kinase inhibitors, carefully follow your healthcare provider's instructions about how to slowly decrease (taper) your dose or stop the other kinase inhibitor medicines before you begin taking Vonjo.
• Vonjo is usually taken by mouth 2 times each day.
• Swallow Vonjo capsules whole. Do not open, break, or chew capsules.
• You can take Vonjo with or without food.
• Take your Vonjo doses at about the same time every day.
• If you notice any change in how often you have bowel movements, if they become softer or you have diarrhea, start taking an antidiarrheal medicine (for example, loperamide) as soon as you notice changes, as directed by your healthcare provider.
• If you take too much Vonjo, call your healthcare provider or go to the nearest emergency room right away and take your bottle of Vonjo with you.
• If you miss a dose of Vonjo, skip the dose and just take your next dose at your regularly scheduled time. Do not take 2 doses at the same time to make up for the missed dose.
• Your healthcare provider will do blood tests before you start taking Vonjo and as needed during treatment.
• Your healthcare provider may change your dose or how often you take Vonjo, temporarily stop or permanently stop treatment with Vonjo if you have certain side effects.

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

This medicine is available in fallowing doasage form:

• As Capsules: 100 mg

This medicine is available in fallowing brand namesː

• Vonjo

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea and vomiting
• low red blood cell count (anemia)
• swelling of your ankles, legs, and feet

Vonjo may affect fertility in males.

Vonjo can cause serious side effects including:

• Bleeding
• Diarrhea
• Worsening low platelet counts
• Changes in the electrical activity of your heart called QTc prolongation
• Increased risk of major cardiovascular events
• Increased risk of blood clots
• Possible increased risk of new (secondary) cancers
• Risk of Infection

What special precautions should I follow?

• Serious and fatal hemorrhages have occurred in Vonjo-treated patients. Avoid use in patients with active bleeding and hold Vonjo prior to any planned surgical procedures. May require dose interruption, dose reduction or permanent discontinuation depending on severity.
• Vonjo causes diarrhea. Manage significant diarrhea with anti-diarrheals, dose reduction, or dose interruption.
• Vonjo can cause worsening thrombocytopenia. Manage by dose reduction or interruption. Monitor platelet count prior to Vonjo treatment and as clinically indicated during treatment [see Dosage and Administration (2.2)]. Interrupt Vonjo in patients with clinically significant worsening of thrombocytopenia that lasts for more than 7 days.
• Vonjo can cause prolongation of the QTc interval. Avoid use in patients with baseline QTc >480 msec. Interrupt and reduce Vonjo dosage in patients who have a QTcF >500 msec. Correct hypokalemia prior to and during Vonjo administration.
• Another Janus associated kinase (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 Vonjo is not indicated. Risk may be increased in current/past smokers and patients with other cardiovascular risk factors. Monitor for signs, evaluate and treat promptly.
• Another JAK-inhibitor has increased the risk of thrombosis, including deep venous thrombosis, pulmonary embolism, and arterial thrombosis (compared to those treated with TNF blockers) in patients with rheumatoid arthritis, a condition for which Vonjo is not indicated. Monitor for signs, evaluate and treat promptly.
• Lymphoma and other malignancies may occur. Past/current smokers may be at increased risk.
• Another JAK-inhibitor increased the risk of serious infections (compared to best available therapy) in patients with myeloproliferative neoplasms. Serious bacterial, mycobacterial, fungal and viral infections may occur in patients treated with Vonjo. Delay starting Vonjo until active serious infections have resolved. Observe for signs and symptoms of infection and manage promptly.
• Co-administration of Vonjo with strong CYP3A4 inhibitors or inducers is contraindicated. Avoid concomitant use of Vonjo with moderate CYP3A4 inhibitors or inducers.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• gastrointestinal toxicities
• myelosuppression
• blurred vision
• dizziness
• worsening performance status
• sepsis

Management of overdosage:

• There is no known antidote for overdose with Vonjo.
• Hemodialysis is not expected to enhance the elimination of Vonjo.

Can this medicine be used in pregnancy?

• It is not known if Vonjo will harm your unborn baby.
• There are no available data on Vonjo use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

Can this medicine be used in children?

• It is not known if Vonjo is safe and effective in children.

What are the active and inactive ingredients in this medicine?

• Active ingredient: pacritinib
• Inactive ingredients: microcrystalline cellulose, polyethylene glycol 8000 (PEG 8000), and magnesium stearate. The capsule shell contains gelatin, titanium dioxide, black iron oxide, erythrosine, red iron oxide and printing ink containing shellac, titanium dioxide, propylene glycol, sodium hydroxide, and povidone.

Who manufactures and distributes this medicine?

Manufactured and Marketed by:

• CTI BioPharma Corp., 3101 Western Ave #800, Seattle WA 98121
• Vonjo is a trademark of CTI BioPharma Corp.

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

• Store Vonjo at room temperature, below 86°F (30°C).
• Store Vonjo in the original package.
• Keep the bottle tightly closed to protect Vonjo from light.

• Dailymed label info on Pacritinib
• FDA Pacritinib

Pacritinib Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

Pacritinib Resources
Latest articles Most recent articles Ongoing trials	Wikipedia