Pacritinib (Systemic)
Brand names: Vonjo
Drug class:
Antineoplastic Agents
Usage of Pacritinib (Systemic)
Intermediate- or High-Risk Myelofibrosis
Treatment of adults with intermediate- or high-risk primary or secondary (post-polycythemia vera or post-essential thrombocythemia) myelofibrosis with a platelet count <50,000/mm3.
Approved under accelerated approval based on proportion of patients achieving ≥35% reduction from baseline in spleen volume; continued approval may be contingent upon verification and description of clinical benefit in cOnfirmatory trials(s).
Designated an orphan drug by FDA for this use.
Myelofibrosis drug treatment is based upon prognostic risk models. Observation alone is advised for asymptomatic low-risk patients; for patients with higher-risk disease, allogeneic hematopoietic stem cell transplant (ASCT) is the preferred treatment. In patients who are not candidates for transplant, JAK inhibitors (i.e., ruxolitinib, Pacritinib, Fedratinib) may be used to provide symptom-based management and improve quality of life.
The first JAK inhibitors approved for myelofibrosis (e.g., ruxolitinib, feratinib) are associated with significant risks of hematologic toxicities. Pacritinib is an additional therapeutic option for patients with symptomatic myelofibrosis who have severe thrombocytopenia. Specific indications and toxicity profiles of the currently available JAK2 inhibitors differ; treatment should be individualized.
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How to use Pacritinib (Systemic)
General
Pretreatment Screening
Patient Monitoring
Other General Considerations
Administration
Oral Administration
Administer orally; take with or without food.
Swallow whole; do not open, break, or chew the capsules.
If a dose is missed, the dose should be taken at the next scheduled time. Do not take an additional dose.
DoSage
Available as pacritinib citrate; dosage expressed in terms of pacritinib.
Adults
Intermediate- or High-Risk Myelofibrosis Oral200 mg twice daily.
Dosage Modification for Toxicity OralIf adverse Reactions occur during pacritinib therapy, temporary interruption of therapy, dosage reduction, and/or discontinuance of the drug may be necessary. If dosage reduction is required, the dosage of pacritinib should be reduced as described in Table 1.
Table 1: Recommended Dosage Reduction for Pacritinib Toxicity.1Dose Reduction Level
Dosage Reduction after Recovery from Toxicity (Initial Dosage = 200 mg twice daily)
First
100 mg twice daily
Second
100 mg once daily
Third
Discontinue drug
The following table indicates the recommended dosage modification (i.e., temporary interruption of therapy, dosage reduction, discontinuance of therapy) for certain adverse effects according to severity.
Table 2. Dosage Modification for Pacritinib Toxicity.1Adverse Reaction and Severity
Modification
Diarrhea
New onset: Initiate anti-diarrheal medications; encourage adequate oral hydration
Grade 3 or 4: Withhold therapy until diarrhea improves to grade 1 or lower; resume at last given dose. Intensify antidiarrheal medications and provide fluid replacement. If diarrhea recurs, withhold therapy until resolution to grade 1 or lower or baseline; resume therapy at 50% of the last dose once toxicity has resolved. Concomitant antidiarrheal treatment is required for patients resuming drug.
Thrombocytopenia
Clinically significant worsening of thrombocytopenia that lasts >7 days: Withhold therapy until thrombocytopenia resolves; resume at 50% of the last dosage. If toxicity recurs, withhold therapy until thrombocytopenia resolves; resume at 50% of the last dosage.
Hemorrhage
Moderate bleeding; intervention indicated: Withhold therapy until bleeding resolves; resume at SAMe dosage. If hemorrhage recurs, withhold therapy until bleeding resolves; resume at 50% of the last dosage
Severe bleeding; transfusion, invasive intervention, or hospitalization indicated: Withhold therapy until bleeding resolves; resume at 50% of the last dosage. If bleeding recurs, discontinue therapy.
Life-threatening bleeding; urgent intervention indicated: Discontinue therapy.
Prolonged QT Interval
QTc prolongation >500 msec or >60 msec from baseline: Withhold therapy. If QTc prolongation resolves to ≤480 msec or baseline within 1 week, resume at same dosage; If time to resolution is >1 week, resume therapy at a reduced dosage.
Special Populations
Hepatic Impairment
No specific dosage recommendations for patients with hepatic impairment.
Patients with Child-Pugh class B: Avoid use.
Patients with Child-Pugh class C: Avoid use.
Renal Impairment
No specific dosage recommendations for patients with renal impairment.
Patients with eGFR (MDRD) <30 mL/minute: Avoid use.
Geriatric Use
No specific dosage recommendations for geriatric patients.
Warnings
Contraindications
Warnings/Precautions
Hemorrhage
Serious and fatal hemorrhage reported in patients with platelet counts <100,000/mm3.
Dosage reduction, interruption, or permanent discontinuation may be required.
Avoid use in patients with active bleeding.
Hold 7 days prior to any planned surgical or invasive procedures.
Assess platelet counts periodically, as clinically indicated.
Manage hemorrhage using treatment interruption and medical intervention.
Diarrhea
Diarrhea occurs frequently; median time to resolution was 2 weeks. Incidence decreases over time; treatment interruption may be necessary.
Control pre-existing diarrhea before starting treatment. Manage with antidiarrheal medications, fluid replacement, and dosage modification.
Treat with antidiarrheal medications promptly at the first onset of symptoms. Interrupt or reduce dosage in patients with significant diarrhea despite optimal supportive care.
Thrombocytopenia
Worsening thrombocytopenia reported. Pacritinib interruption and dosage reduction may be required.
Monitor platelet count prior to treatment and as clinically indicated during treatment.
Interrupt pacritinib in patients with clinically significant worsening of thrombocytopenia that lasts for >7 days. Once the toxicity has resolved, restart at 50% of the last given dosage.
If toxicity recurs, hold pacritinib; resume the drug at 50% of the last given dose once the toxicity has resolved.
Prolonged QT Interval
Can cause prolongation of the QTc interval. QTc prolongation of >500 msec or increase from baseline by ≥60 msec was higher in pacritinib-treated patients than patients in the control group.
Adverse reactions related to QTc prolongation reported; no cases of torsades de pointes reported.
Avoid use in patients with a baseline QTc of >480 msec. Avoid concomitant use of drugs with significant potential for QTc prolongation.
Correct hypokalemia prior to and during treatment. Manage QTc prolongation with dose interruption and electrolyte management.
Major Adverse Cardiac Events (MACE)
Increased risk of major adverse cardiovascular events (MACE), including cardiovascular death, MI, and stroke, reported in patients receiving other JAK inhibitors for the treatment of rheumatoid arthritis.
Consider risks and benefits of pacritinib prior to initiating or continuing therapy, particularly in patients who are current or past smokers and in those with other cardiovascular risk factors. Advise patient to seek immediate medical attention if symptoms of serious cardiovascular events occur.
Thromboembolic Events
Serious and sometimes fatal thromboembolic events, including DVT, PE, and arterial thrombosis in the extremities, reported in patients receiving other JAK inhibitors for the treatment of rheumatoid arthritis.
Promptly evaluate and treat any patients who develop symptoms of thrombosis during treatment with pacritinib.
Secondary Malignancies
Another JAK inhibitor increased risk of lymphoma and other malignancies, excluding non-melanoma skin cancer (NMSC), in patients with rheumatoid arthritis.
Consider risks and benefits of pacritinib prior to initiating therapy or when considering whether to continue pacritinib, particularly in patients with a known malignancy (other than successfully treated NMSC), in those who develop a malignancy, and those who are current or past smokers.
Risk of Infection
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.
Resolve active serious infections prior to initiating pacritinib. Observe patients for signs and/or symptoms of infection and promptly initiate appropriate treatment.
Employ active surveillance and prophylactic antibiotics according to clinical guidelines.
Interactions with CYP3A4 Inhibitors or Inducers
Concomitant use with strong CYP3A4 inhibitors or inducers contraindicated.
Avoid concomitant use with moderate CYP3A4 inhibitors or inducers.
Specific Populations
PregnancyAnimal studies revealed maternal toxicity and embryonic and fetal loss at dosages considerably lower than the recommended human dose.
No available human data to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes related to the use of pacritinib.
Advise pregnant women of the potential risk to a fetus. Consider benefits and risks of pacritinib for the mother and possible risks to the fetus when prescribing pacritinib to a pregnant woman.
LactationNo data on presence of pacritinib in either human or animal milk, effects on the breast-fed child, or effects on milk production.
Females should not breast-feed while receiving the drug, and for at least 2 weeks after the last dose.
Females and Males of Reproductive PotentialReduced male mating and fertility in mice. Pacritinib may impair male fertility in humans.
Pediatric UseSafety and efficacy not established.
Geriatric UseExperience in patients ≥65 years of age is insufficient to determine whether geriatric patients respond differently than younger individuals.
Hepatic ImpairmentMild (Child-Pugh class A): AUC decreased by 8.5%.
Moderate (Child-Pugh class B): AUC decreased by 36%. Avoid use.
Severe hepatic impairment (Child-Pugh class C): AUC decreased by 45%. Avoid use.
Renal ImpairmenteGFR 15 to 29 mL/minute: Peak plasma concentration and AUC of pacritinib increased by approximately 30%. Avoid use.
eGFR <15 mL/minute on hemodialysis: Peak plasma concentration and AUC of pacritinib increased by approximately 30%. Avoid use.
Common Adverse Effects
Adverse effects (≥20%): Diarrhea, thrombocytopenia, nausea, anemia, peripheral edema.
What other drugs will affect Pacritinib (Systemic)
Metabolized mainly by CYP3A4.
Pacritinib inhibits CYP1A2, 2C19 and 3A4 and to a lesser extent CYP1A2, 2B6, 2C8, 2C9, and 2D6.
Pacritinib is an inducer of CYP1A2 and 3A4.
Pacritinib is not a substrate of breast cancer resistance protein (BCRP), multidrug resistance-associated protein (MRP) 2, organic anion-transporters (OAT) 1 and 3, organic anion-transporting polypeptides (OATP) 1B1 and 1B3, organic cation transporters (OCT) 1 and 2, or P-glycoprotein (P-gp).
Pacritinib is an inhibitor of BCRP, OCT1, OCT2, and P-gp, but not an inhibitor of bile salt export pump (BSEP), MRP2, OAT1, or OAT3.
Drugs Affecting Hepatic Microsomal Enzymes
Potent CYP3A4 inhibitors: Pharmacokinetic interaction (increased pacritinib peak plasma concentrations and AUC). Concomitant use is contraindicated.
Moderate CYP3A4 inhibitors: Pharmacokinetic interaction not studied. Avoid.
Potent CYP3A4 inducers: Pharmacokinetic interaction (decreased pacritinib peak plasma concentrations and AUC). Concomitant use is contraindicated.
Moderate CYP3A4 inducers: Pharmacokinetic interaction not studied. Avoid.
Drugs Metabolized by Hepatic Microsomal Enzymes
CYP1A2 substrates: Pharmacokinetic interaction (increased substrate plasma concentration). Avoid co-administration.
CYP 3A4 substrates: Pharmacokinetic interaction (increased substrate plasma concentration). Avoid co-administration.
Drugs Affecting or Affected by Transport Systems
P-gp substrates: Pharmacokinetic interaction (increased substrate plasma concentration). Avoid co-administration.
BCRP substrates: Pharmacokinetic interaction (increased substrate plasma concentration). Avoid co-administration.
OCT1 substrates: Pharmacokinetic interaction (increased substrate plasma concentration). Avoid co-administration.
Drugs Associated with QT Prolongation
Avoid co-administration of drugs with significant potential for QTc prolongation with pacritinib.
Specific Drugs and Foods
Drug
Interaction
Comments
Clarithromycin
Increased peak plasma concentrations (by 30%) and AUC (by 80%)
Contraindicated. Avoid concomitant use
Rifampin
Decreased peak plasma concentrations (by 51%) and AUC (by 87%)
Contraindicated. Avoid concomitant use
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