Pomalidomide – Targeted Therapy
Pomalidomide is a third-generation antitumor immunomodulator belonging to the IMiDs group (thalidomide derivatives). The drug possesses potent direct cytotoxic and mediated immune effects, making it highly effective in treating refractory forms of hematological malignancies.
The mechanism of action of pomalidomide is linked to its binding to the cereblon protein (CRBN), which is part of the E3 ubiquitin ligase enzymatic complex. This leads to the selective degradation of specific proteins (Ikaros and Aiolos) required for the survival of malignant B-cells. Consequently, tumor growth is inhibited, apoptosis is induced, and the activity of T-cells and natural killer (NK) cells is enhanced, allowing them to attack cancer cells more effectively. The drug also blocks the production of pro-inflammatory cytokines and suppresses angiogenesis within the bone marrow.
The drug is intended for oral administration and is typically used in cases where other therapies, including lenalidomide and bortezomib, have failed.
Indications
Pomalidomide is used in hemato-oncology for the therapy of the following conditions:
- Relapsed and Refractory Multiple Myeloma: in combination with dexamethasone for adult patients who have received at least two prior treatment lines.
- Kaposi Sarcoma: in patients with HIV infection when highly active antiretroviral therapy (HAART) is ineffective, or in HIV-negative patients with advanced disease.
Dosage and administration
The pomalidomide dosing regimen is established by a physician based on the patient's condition and blood counts.
- Standard Dose: typically 4 mg once daily.
- Cycling: the drug is taken for 21 days, followed by a 7-day break (28-day cycle).
- Administration Rules: capsules are taken orally at the same time each day, without chewing or opening, regardless of food intake.
- Monitoring: complete blood count monitoring is required before the start of each cycle (neutrophil count must be ≥ 1,000/mm³).
- Dose Adjustment: if neutropenia or thrombocytopenia develops, the dosage may be reduced to 3 mg, 2 mg, or 1 mg.