Generic
Pomalidomide
2 brands available in the market
At a glance
Pomalidomide is used for the treatment of multiple myeloma and Kaposi sarcoma. It is a thalidomide analogue with immunomodulatory, antiangiogenic, and antineoplastic properties.
Description
Pomalidomide is an analogue of thalidomide with immunomodulatory, antiangiogenic, and antineoplastic properties. Its cellular activities are mediated through cereblon, a component of a cullin ring E3 ubiquitin ligase enzyme complex. In vitro, it inhibits proliferation and induces apoptosis of hematopoietic tumor cells. It enhances T cell- and NK cell-mediated immunity and inhibits production of pro-inflammatory cytokines.
Indications
- Multiple myeloma (in combination with dexamethasone, after at least 2 prior therapies)
- AIDS-related Kaposi sarcoma (after HAART failure)
- Kaposi sarcoma in HIV-negative adults
Therapeutic class
Targeted Cancer Therapy
Pharmacological class
Immunomodulator (Cereblon Ligand)
Pharmacology
Pomalidomide binds to cereblon, a component of an E3 ubiquitin ligase complex. It targets substrate proteins (including Aiolos and Ikaros) for ubiquitination and subsequent degradation, leading to cytotoxic and immunomodulatory effects. It enhances T cell- and NK cell-mediated immunity and inhibits pro-inflammatory cytokine production.
Mechanism of action
Exerts anticancer effects through cereblon-mediated protein degradation and immune system activation.
Dosage
Adult Dose (Oral):
- Multiple myeloma: 4 mg once daily (Days 1-21 of 28-day cycle), with dexamethasone
- Kaposi sarcoma: 5 mg once daily (Days 1-21 of 28-day cycle)
- With strong CYP1A2 inhibitors: Reduce dose to 2 mg
- Dose modifications for hematologic adverse reactions
Administration
- May be taken with or without food
- Take at the same time each day
- Pregnancy testing and contraception required
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects (>30%):
- Multiple myeloma: Fatigue/asthenia, neutropenia, anemia, constipation, nausea, diarrhea, dyspnea, upper respiratory tract infections, back pain, pyrexia
- Kaposi sarcoma: Decreased neutrophils/WBC, elevated creatinine/glucose, rash, constipation, fatigue, decreased hemoglobin/platelets/phosphate/albumin/calcium, elevated ALT, nausea, diarrhea
Precautions & warnings
- Increased mortality observed with pembrolizumab + dexamethasone + thalidomide analogue
- Hematologic toxicity (neutropenia most common Grade 3/4); monitor
- Hepatotoxicity (hepatic failure including fatalities); monthly liver function tests
- Discontinue for severe cutaneous reactions
- Monitor for tumor lysis syndrome in high tumor burden patients
- Discontinue for angioedema and anaphylaxis
- Potential fetal harm; effective contraception required
Contraindications
- Pregnant females
- Hypersensitivity to pomalidomide or any ingredient
Drug interactions
- Strong CYP1A2 inhibitors: Avoid concomitant use; if unavoidable, reduce dose to 2 mg
Food interactions
It is not known whether it is safe to consume alcohol with Pomalidomide.
Use in pregnancy
Use in Pregnancy: Contraindicated in pregnancy; can cause fetal harm; teratogenic during organogenesis.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: No information on presence in human milk; due to potential adverse reactions, advise women not to breastfeed during treatment.
Pediatric use
Safety and effectiveness not established in pediatric patients.
Geriatric use
No dose adjustment required for elderly patients.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment may be needed; consult your doctor.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed; consult your doctor.
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Store below 30°C, away from light and moisture; keep out of reach of children.
Chemical structure
Pomalidomide