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
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.
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.
Contraindications
- Pregnant females
- Hypersensitivity to pomalidomide or any ingredient
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
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.
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
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.
Therapeutic class
Targeted Cancer Therapy
Storage conditions
Store below 30°C, away from light and moisture; keep out of reach of children.
Chemical structure
Pomalidomide