Pomalyst

Multiple myeloma — in combination with dexamethasone in patients who have received at least two prior therapies including lenalidomide and a proteasome inhibitor and have demonstrated disease progression on or within 60 days of completion of the last therapy; AIDS-related Kaposi sarcoma — after failure of highly active antiretroviral therapy (HAART) or in those for whom HAART is not an option

Multiple myeloma: 4 mg orally once daily Days 1-21 of 28-day cycle (with dexamethasone 40 mg weekly)
Kaposi sarcoma: 5 mg orally once daily Days 1-21 of 28-day cycle
Take on empty stomach (at least 2 hours before or 2 hours after food)

Capsules: 1 mg, 2 mg, 3 mg, 4 mg

Pregnancy — pomalidomide is an analogue of thalidomide. Available only through POMALYST REMS program.

• Embryo-Fetal Toxicity: REMS required. Two forms of contraception mandatory.
• Venous/Arterial Thromboembolism: DVT, PE, MI, stroke reported. Thromboprophylaxis recommended.
• Hematologic Toxicity: Neutropenia (50% Grade 3-4), anemia (25%), thrombocytopenia (22%). Monitor CBC weekly for first 8 weeks then monthly.
• Hepatotoxicity: Elevated ALT/AST reported. Monitor LFTs monthly.
• Severe Cutaneous Reactions: SJS, TEN, DRESS reported. Discontinue permanently.
• Tumor Lysis Syndrome: Fatal cases reported. Monitor at-risk patients.
• Dizziness and Confusional State: Advise patients not to drive or operate machinery.
• Second Primary Malignancies: Observed in clinical trials.

Fatigue (55%), neutropenia (52%), anemia (38%), constipation (36%), nausea (36%), diarrhea (34%), dyspnea (34%), upper respiratory tract infection (32%), back pain (25%), pyrexia (19%), bone pain (16%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Pomalidomide is an immunomodulatory agent with direct anti-myeloma tumoricidal activity, immune modulation, and stromal cell interaction inhibition. It binds to cereblon (CRBN), leading to enhanced ubiquitination and proteasomal degradation of the transcription factors Ikaros (IKZF1) and Aiolos (IKZF3). It also inhibits angiogenesis, enhances T-cell and NK-cell mediated immunity, and inhibits production of pro-inflammatory cytokines.

Tmax: 2-3 hours. Half-life: approximately 7.5 hours. Protein binding: 12-44%. Metabolized by CYP1A2 and CYP3A4. Excreted in urine (73%, 2% unchanged) and feces (15%). No dose adjustment for renal impairment.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• MM-003 — Pomalidomide + low-dose dex vs. high-dose dex in relapsed/refractory MM. Phase III, n=455.
  🔬 NCT01311687 ↗ 📄 Primary Publication ↗

Pomalyst has FDA-approved indications across the following cancer types covered on PipelineEvidence: