Revlimid (Lenalidomide)

General Information

Antineoplastic drug, immunomodulator Relvimid (Lenalidomid) has both immunomodulatory, and antiangiogenic properties. It inhibits secretion of pro-inflammatory cytokine, including FNO, interleukin-1 (IL-1), IL-6 and IL-12, from liposaccharide (LPS) – the stimulated peripheral mononuclear blood cells (PMBC).

Relvimid stimulates production of anti-inflammatory cytokina of SILT-10 from LPS-stimulated PMKK and an expression inhibition and fermental activity of TsOG-2.

Relvimid – Lenalidomide induces proliferation of T-cages and increases synthesis of SILT-2 and interferon-1 and also increases cytotoxic activity of own cell killers. It inhibits proliferation of cells of various lines of haemopoetic tumors, mainly those which have cytogenetic defects of a chromosome 5.

On model of differentiation of endothelial cells predecessors Relvimid induces an expression of fetal hemoglobin, depending on differentiation of CD34+ of stem haemopoetic cells.

Relvimid inhibits angiogenesis, blocking formation of microvessels and endothelial channels and also migration of endothelial cells on model of angiogenesis in vitro. Besides, Relvimid inhibits synthesis of a proangiogen vascular endothelial factor of growth by means of RS-3 of a prostate gland tumor cells.

Revlimid (Lenalidomide) is the leading compound of a new class of immunomodulators with antiangiogenic and immunomodulatory properties. Revlimid inhibits secretion of anti-inflammatory cytokine, including a tumor necrosis factor – and (FNO-a), IL-6, interleukin-1 р (IL-1(3) and IL-12, from liposaccharide (LPS) – the stimulated mononuclear peripheral blood cells (PMBC). Revlimid induces proliferation of T-cells and increases synthesis of SILT-2 and interferon – 1u and also increases cytotoxic activity of own cell killers. Revlimid raises production of anti-inflammatory cytokine IL-10 from LPS-stimulated PMKK. This medicine inhibits proliferation of cells of various lines of haemopoetic tumors, mainly those which have cytogenetic defects of a chromosome 5. After intake of the drug it is quickly absorbed; at the same time the maximum concentration is reached in approx. 1 hour after taking. Dietary pattern doesn't influence extent of absorption. Pharmacokinetic distribution is linear. The area under a curve “concentration time” (AUC) increase and the maximum concentration is in proportion to increase in a dose. Repeated intake of the drug doesn't affect its accumulation. Elimination half-life of medicine rises proportional to a dose, approx. from 3 hours at a dose of 5 mg up to about 9 hours at doses of 400 mg. The balance is to be reached on the 4th day. There is no information about the admission of a Revlimid in breast milk. The pharmacokinetics of this drug in patients with liver dysfunction wasn't studied. In patients with kidneys dysfunction, absorption of Revlimid doesn't change. At the same time, recovery of the medicine is slowed down in proportion to the extent of impaired renal function.

Disease

• Multiple myeloma.

Precautions

Revlimid has following contraindications:

• Hypersensitivity to the active substance or any component of Revlimid.
• Women who are able to become pregnant if they do not fulfill all the requirements of the contraceptive program
• Pregnancy and breast feeding period
• Young age (insufficiently clinical experience of application)
• Intolerance to lactose, deficiency of lactase or the broken glucose galactose absorption as capsules contain lactose.

How to take?

Revlimid is prescribed by oncologists, who have experience in the treatment of multiple myeloma, myelodysplastic syndromes or mantle cell lymphoma. Always follow the doctor's instructions and instructions for lenalidomide, if you are not sure, consult your doctor concerning the prescribed doses of Revlimid and other medications in case of combined treatment.

Revlimid is taken on certain days, observing the regime for 4 weeks (28 days). These 28 days are called the treatment cycle. After completing this cycle, a new cycle begins. Revlimid capsules are taken whole, swallowed with a sufficient amount of water, regardless of the intake of food. It is forbidden to break, open and chew capsules. Consult a doctor before starting to take this medicine.

Side-Effects

During the treatment with Revlimid, the patient may experience side effects. Tell your doctor if you experience any of these.

• Pneumonia, upper respiratory tract infection, bacterial, viral infections (including opportunistic infections)
• Nasopharyngitis, bronchitis, pharyngitis
• Acute myelogenous leukemia, myelodysplastic syndrome, squamous cell carcinoma of the skin
• Neutropenia, leukopenia, thrombocytopenia, pancytopenia, anemia, hemorrhagic disorders, febrile neutropenia
• Hypothyroidism
• Hyperglycemia, hypokalemia, hypocalcemia, weight loss, loss of appetite
• Hypomagnesemia, dehydration, hyperuricemia
• Depression, insomnia
• Peripheral neuropathies (excluding motor neuropathy), dizziness, tremor, taste perversion, headache
• Ataxia, imbalance

Before prescribing Revlimid, the doctor has to evaluate all risks and potential benefits of treatment.

Interactions

• Oral contraceptives
• Dexamethasone decreases the effectiveness of contraceptives. For proper pregnancy prevention, use the drugs reommended in the Pregnancy Protection Program
• Digoxin. In case of simultaneous prescription of Revlimid with Digoxin the concentration of Digoxin in plasma increases. This is to be monitored thoroughly.
• Warfarin. Relvimid and Warfarin don’t influence the pharmacokinetic characteristics. While using dexamethasone together with Relvimid, the influence of the latter on the effectiveness of warfarin can’t be excluded. Warfarin concentration is to be carefully monitored.

Overdose

There is no special plan of action for an overdose of lenalidomide in patients with multiple myeloma, despite the fact that in studies on determining the dose range, some patients received doses up to 150 mg, and in studies of single dose exposure up to 400 mg of the drug. Toxic manifestations, which limited the dose in these studies, were exclusively hematological.

In case of an overdose, symptomatic maintenance therapy is recommended.

Efficiency and safety of Revlimid was studied in five Phase III studies of newly diagnosed multiple myeloma, two Phase III studies of relapsing refractory multiple myeloma, one Phase III study and one Phase II study of myelodysplastic syndromes and one Phase II study of mantle cell lymphoma.

Based on the results of all clinical trials, Revlimid demonstrated an improvement in overall survival in patients with newly diagnosed / untreated lymphoma, especially in combination with decadron. Undergoing maintenance therapy with Revlimid, patients achieve long-term remission, the drug significantly increases the time before the progression and overall survival. Therefore, patients are interested in the price of Revlimid and think about where and how to buy it. Because it is a drug that gives hope, if not for full recovery, but at least for the continuation of life and the improvement of its quality.

Reviews

Rita: My grandmother fell ill when she was 60 years old. A multiple myeloma was detected. She consulted a hematologist, and he found that my grandmother has the I stage of multiple myeloma. In the beginning, no therapy was prescribed, they just regularly took tests.
The treatment was strictly under the supervision of a chemotherapist and a hematologist. My grandmother got a standard course of treatment, 28 days long. By the end of the treatment, there were improvements in the condition. Nausea passed, and there was less pain in the legs. Of course, the drug is not cheap, but the result is good. You need to order it in online pharmacies, because it is simply not available in a regular pharmacy.

Sergio: I have been fighting with MM for 2 and a half years already. The first time helped Velcade + Dexymethasone + stem cell transplant. After the remission, as expected, a relapse occurred. After two courses of chemotherapy, it became clear that Velcade helps no longer, and it was impossible to get or buy Revlimid… I was given a pack of Revlimid, the grandmother, which had taken it, died. I bought 2 more packs at an adequate price. We made the 5th course of HT and a stem cell transplant. On December of the 30th, 2013 there was a diagnosis: remission. Now, however, I struggle with a typical complication after HT – herpes zoster, but this is trifles.

Kenny: I got the diagnosis of “multiple myeloma” in 2007. During this time, I did not undergo a treatment course with various drugs. However, the most effective was Revlimid. It gave the greatest effect and resulted in a relief of the disease. It’s a pity that I did not have enough money for further treatment, and I developed resistance to other drugs. Therefore, the effect of Revlimid was, unfortunately, not consolidated.

Berta: For the treatment of multiple myeloma, Revlimid was prescribed for me in combination with Dexamethasone. In the hospital, I often met with the patients with the same diagnose; we exchanged information on treatment and on the process of recovery. Compared with other, I took a smaller dose of Decadron. I can say that my side effects were manifested to a much lesser extent. But the main thing is that we both had no progression of the disease. After the beginning of treatment, I live the second year already. My torment did not end completely, I just got used to living in such a rhythm.

Vladimir: I had a relapsing multiple myeloma. With the prescription of Revlimid it was possible to achieve complete remission when there was no hope of recovery. The course of treatment was long enough and in a certain sense excruciating, but I won several years of life. An excellent feeling when, without hopes, with your hands down, you get a chance to live again. Thanks to the developers of the drug! I hope that in the future it will become much cheaper, and even more people will get a chance for recovery.