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All about: Lenalidomide

Big Image Pronouncation: (LEN-a-LID-oh-mide)
Class: Immunologic agent

Trade Names:
Revlimid
- Capsules 5 mg
- Capsules 10 mg
- Capsules 15 mg
- Capsules 25 mg

Mechanism of Action

Pharmacology

Possesses antineoplastic, immunomodulatory, and antiangiogenic properties.

Pharmacokinetics

Absorption

Rapidly absorbed following oral administration, with C max occurring 0.625 to 1.5 h postdose. Food reduces C max 36%. The pharmacokinetic disposition is linear; C max and AUC increase proportionately with dose. In multiple myeloma patients, C max occurred 0.5 to 4 h after administration.

Distribution

Plasma protein binding approximately 30%.

Elimination

Approximately 67% is excreted unchanged in the urine and exceeds glomerular filtration rate, indicating elimination is partially or entirely active. The t ½ is about 3 h.

Special Populations

Renal Function Impairment

The AUC was 56% greater in multiple myeloma patients with mild renal function impairment compared with healthy renal function.

Indications and Usage

Treatment of patients with transfusion-dependent anemia due to low or intermediate-1 risk myelodysplastic syndromes (MDS) associated with a deletion 5q cytogenetic abnormality, with or without additional cytogenetic abnormalities; treatment of multiple myeloma in combination with dexamethasone in patients who have received at least 1 prior therapy.

Contraindications

Pregnancy; women capable of becoming pregnant; hypersensitivity to any component of the product.

Dosage and Administration

MDS
Adults

PO 10 mg once daily.

Dosage Adjustments Due to Thrombocytopenia If thrombocytopenia develops within 4 wk of starting treatment at 10 mg once daily

Interrupt lenalidomide when platelets fall to fewer than 50,000/mcL, then resume lenalidomide at 5 mg once daily when platelets return to 50,000/mcL or more.

Interrupt lenalidomide when platelets fall to 50% of baseline value

Resume lenalidomide at 5 mg once daily if baseline was 60,000/mcL or greater and returns to 50,000/mcL or more, or if baseline is less than 60,000/mcL and returns to 30,000/mcL or more.

If thrombocytopenia develops after 4 wk of starting treatment at 10 mg once daily

Interrupt lenalidomide when platelets fall to less than 30,000/mcL, or less than 50,000/mcL and platelet transfusions, then resume lenalidomide at 5 mg once daily when platelets return to 30,000/mcL or more (without hemostatic failure).

If thrombocytopenia develops during treatment at 5 mg once daily

Interrupt lenalidomide when platelets fall to less than 30,000/mcL, or less than 50,000/mcL and platelet transfusions, then resume lenalidomide at 5 mg every other day when platelets return to 30,000/mcL or more (without hemostatic failure).

Dosage Adjustments Due to Neutropenia If neutropenia develops within 4 wk of starting treatment at 10 mg once daily

Interrupt lenalidomide when absolute neutrophil count (ANC) falls to less than 750/mcL, then resume lenalidomide at 5 mg once daily when neutrophils return to 1,000/mcL or more. Interrupt lenalidomide when neutrophils fall to less than 500/mcL, then resume lenalidomide at 5 mg once daily when neutrophils return to 500/mcL or more.

If neutropenia develops after 4 wk of starting treatment at 10 mg once daily

Interrupt lenalidomide when neutrophils fall to less than 500/mcL for 7 days or more, or less than 500/mcL and associated with fever (101.3°F or higher), then resume lenalidomide at 5 mg once daily when neutrophils return to 500/mcL or more.

If neutropenia develops during treatment at 5 mg once daily

Interrupt lenalidomide when neutrophils fall to less than 500/mcL for 7 days or more, or less than 500/mcL and associated with fever (101.3°F or higher), then resume lenalidomide at 5 mg every other day when neutrophils return to 500/mcL or more.

Multiple Myeloma
Adults

PO 25 mg once daily on days 1 to 21 of repeated 28-day cycles.

Dosage Adjustments Due to Thrombocytopenia

Interrupt treatment, follow CBC weekly when platelets fall to less than 30,000/mcL, resume treatment at 15 mg/day when platelets return to 30,000/mcL or more. Interrupt treatment for each subsequent platelet drop to less than 30,000/mcL, resume treatment at 5 mg less than the previous dose. When platelets return to 30,000/mcL or more, do not dose below 5 mg daily.

Dosage Adjustments Due to ANC

Interrupt treatment, add granulocyte colony–stimulating factor, and follow CBC weekly when neutrophils fall to less than 1,000/mcL, then resume treatment at 25 mg daily when neutrophils return to 1,000/mcL or more and neutropenia is the only toxicity; however, if there is other toxicity, resume treatment at 15 mg daily. Interrupt treatment for each subsequent drop in neutrophils below 1,000/mcL, then resume treatment at 5 mg less than the previous dose when neutrophils are 1,000/mcL or greater. Do not dose below 5 mg/day.

Other Grade 3/4 toxicities

For other grade 3/4 toxicities related to lenalidomide, hold treatment and restart at the next lower dose level when toxicity has resolved to grade 2 or less.

General Advice

  • Administer prescribed dose once daily with water. Administer without regard to meals but with food if GI upset occurs.
  • Instruct patient not to break, chew, or open the capsule.
  • If a dose is missed, administer as soon as possible on that day. If the dose is missed for an entire day, administer the next dose at the regularly scheduled time. Do not double the dose to catch up.

Storage/Stability

Store capsules at 59° to 86°F.

Drug Interactions

Digoxin

Digoxin C max is increased 14% with coadministration.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension (6%); palpitations (5%); aggravated atrial fibrillation, angina pectoris, aortic disorder, atrial fibrillation, bradycardia, cardiac arrest, cardiac failure, cardiogenic shock, cardiomyopathy, cardiorespiratory arrest, congestive cardiac failure, deep vein thrombosis (DVT), hypotension, ischemia, MI, myocardial ischemia, pulmonary edema, superficial thrombophlebitis, supraventricular arrhythmia, tachyrhythmia, thrombosis, transient ischemic attack, ventricular dysfunction.

CNS

Fatigue (31%); pyrexia (21%); dizziness, headache (20%); asthenia (15%); insomnia (10%); hyposthesia (7%); dysgeusia (6%); depression, peripheral neuropathy (5%); abnormal gait, aphasia, cerebellar infarction, cerebrovascular accident, confusional state, depressed level of consciousness, dysarthria, migraine, spinal cord compression, subarachnoid hemorrhage.

Dermatologic

Pruritus (42%); rash (36%); dry skin (14%); contusion, night sweats (8%); increased sweating (7%); ecchymosis, erythema (5%); acute febrile neutrophilic dermatosis.

EENT

Nasopharyngitis (23%); pharyngitis (16%); rhinitis (7%); ear infection, vertigo.

Endocrine

Hypothyroidism (7%); Basedow disease, dehydration, gout, hypernatremia, hypoglycemia.

GI

Diarrhea (49%); constipation, nausea (24%); abdominal pain (12%); vomiting (10%); upper abdominal pain (8%); dry mouth (7%); loose stools (6%); colonic polyp, diverticulitis, dysphagia, gastritis, gastroenteritis, gastroesophageal reflux disease, GI hemorrhage, intestinal perforation, irritable bowel syndrome, ischemic colitis, melena, obstructive inguinal hernia, pancreatitis, pancreatitis due to biliary obstruction, perirectal abscess, rectal hemorrhage, small intestinal obstruction, upper GI hemorrhage.

Genitourinary

UTI (11%); dysuria (7%), azotemia, blood creatinine increase, hematuria, kidney infection, renal failure, renal mass, ureteric calculus.

Hematologic-Lymphatic

Thrombocytopenia (62%); neutropenia (59%); anemia (12%); leukopenia (8%); febrile neutropenia (5%); bone marrow depression, coagulopathy, hemoglobin decreased, hemolysis, hemolytic anemia, refractory anemia, splenic infarction, warm-type hemolytic anemia.

Hepatic

Acute cholecystitis, cholecystitis, hepatic failure, hyperbilirubinemia, LFTs abnormal.

Lab Tests

Increased ALT (8%); troponin Ι increased.

Metabolic-Nutritional

Hypokalemia (11%); anorexia (10%); hypomagnesemia (6%).

Musculoskeletal

Arthralgia (22%); back pain (21%); muscle cramp (18%); limb pain (11%); myalgia (9%); peripheral swelling (8%); rigors (6%); arthritis, bone fractures, chondrocalcinosis pyrophosphate, fall, gouty arthritis, neck pain.

Respiratory

Cough (20%); dyspnea (17%); epistaxis, upper respiratory tract infection (15%); pneumonia (12%); sinusitis (8%); exertional dyspnea (7%); bronchitis (6%); acute sinusitis, chronic obstructive airway disease exacerbated, interstitial lung disease, lobar pneumonia, lung infiltration, respiratory failure, wheezing.

Miscellaneous

Peripheral edema (20%); edema (10%); pain (7%); cellulitis, chest pain (5%); bacteremia, central line infection, clostridial infection, disease progression (culture negative), Enterobacter sepsis, fungal infection, herpes viral infection, hypersensitivity, infection, influenza, intermittent pyrexia, Klebsiella sepsis, localized infection, neoplasm (eg, acute leukemia, acute myeloid leukemia, bronchoalveolar carcinoma, lymphoma, metastatic lung cancer, metastatic prostate cancer), nodule, oral infection, overdose, pelvic pain, postprocedural hemorrhage, Pseudomonas infection, road traffic accident, septic shock, staphylococcal infection, sudden death, transfusion reaction.

Precautions

Warnings

Potential for human birth defects

Lenalidomide is an analog of thalidomide, a known human teratogen that causes severe, life-threatening human birth defects. If lenalidomide is taken during pregnancy, it may cause birth defects or death to the fetus. Advise women to avoid becoming pregnant while taking lenalidomide. Lenalidomide is only available under a restricted distribution system in which only health care providers and pharmacists registered with the program are able to prescribe and dispense lenalidomide; only patients who are registered and meet all the requirements of the program are able to receive the medication.

Hematologic toxicity

Significant neutropenia and thrombocytopenia can develop in patients with deletion 5q MDS. Lenalidomide dose reduction/delay may be necessary. Patients may require use of blood product support and/or growth factors. Monitor CBC weekly for first 8 wk of therapy and at least monthly thereafter.

DVT and pulmonary embolism (PE)

Increased risk of DVT and PE exists in patients with multiple myeloma treated with lenalidomide combination therapy. It is not known if prophylactic anticoagulation or antiplatelet therapy may reduce the potential for venous thromboembolic events.


Monitor

Perform CBC, including WBC count with differential, platelet count, Hgb, and Hct, weekly for first 8 wk of therapy and at least monthly thereafter to monitor for cytopenias.


Pregnancy

Category X .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Patients 65 yr of age and older experience more frequent serious adverse reactions. Because elderly patients are more likely to have decreased renal function, take care in dose selection and monitor renal function.

Renal Function

Risk of adverse reactions may be increased. Take care with dose selection and monitor renal function.

Men

Contraindicated in sexually mature men unless patient meets the following conditions: understands the risks associated with the drug and is thought to be able to reliably carry out instructions; is capable of complying with the contraceptive measures that are appropriate for men, patient registration, and patient survey as described in the RevAssist program; has received oral and written warnings of potential risks of taking lenalidomide and exposing a fetus to the drug; has received oral and written warnings of the risk of possible contraception failure and that it is unknown whether lenalidomide is present in semen, and of the need for barrier contraception (latex condoms even with successful vasectomy); acknowledges in writing understanding of these warnings and of need to use a latex condom during any sexual contact with women of childbearing potential; parent or legal guardian reads the educational materials and agrees to try to ensure compliance with above for patients between 12 and 18 yr of age.

Pregnancy testing

During therapy and during dose interruptions, pregnancy testing should occur weekly during first 4 wk of use, then every 4 wk in women with regular menstrual cycles, or every 2 wk in women with irregular menstrual cycles. Perform pregnancy testing if a patient misses a monthly menstrual cycle or if there is any abnormality in her pregnancy test or menstrual bleeding. Discontinue lenalidomide during this evaluation.

Women

Contraindicated in women of childbearing potential unless alternative therapies are inappropriate and patient meets the following conditions: understands the risks associated with the drug and is thought to be able to carry out instructions; is capable of complying with the contraceptive measures, pregnancy testing, patient registration, and patient survey as described in the RevAssist program; has received both oral and written warnings of potential risks of taking lenalidomide during pregnancy and of exposing a fetus to the drug; has received oral and written warnings of the risk of possible contraception failure and of the need to use 2 reliable forms of contraception simultaneously, unless continuous abstinence from heterosexual sexual contact is the chosen method. Sexually mature women who have not undergone a hysterectomy or who have not been menopausal for at least 24 consecutive months (have had menses at some time in the preceding 24 consecutive months) are considered to be of childbearing potential; acknowledges in writing the understanding of these warnings and of need for using 2 reliable methods of contraception for 1 mo prior to starting lenalidomide therapy, during therapy, during dose interruption, and for 1 mo after stopping therapy; has had 2 negative pregnancy tests with a sensitivity of at least 50 milliunits/mL, within 10 to 14 days and 24 h prior to beginning therapy; parent or legal guardian reads the educational materials and agrees to try to ensure compliance with above for patients between 12 and 18 yr of age.

Overdosage

Symptoms

None reported.

Patient Information

  • Review guidelines and requirements for participation in the RevAssist program with patient or caregiver.
  • Advise patient or caregiver to read the Medication Guide carefully before starting therapy and to read and each time the medication is refilled.
  • Advise patient that regular blood tests will be required during treatment and that the dose of the medication may be adjusted or treatment interrupted based on results of blood tests and patient's general condition.
  • Advise patient that medication will only be dispensed in a 28-day supply at one time, and that he/she must comply with the RevAssist program requirements for monitoring, including pregnancy tests for women of childbearing potential, before the medication can be refilled.
  • Instruct patient to take prescribed dose with a glass of water once daily. Advise patient that medication can be taken without regard to meals but to take with food if stomach upset occurs.
  • Caution patient to swallow capsules whole and not to break, chew, or open the capsules.
  • Advise patient that if a dose is missed to take it as soon as remembered that day. Instruct patient that if dose is missed for an entire day not to take the missed dose, but take the next dose at the regularly scheduled time; advise patient not to double the dose to catch up.
  • Instruct patient not to change the dose or stop taking unless advised by health care provider.
  • Instruct patient to immediately seek medical care if any of the following occur: bleeding or unusual bruising; fever, sore throat, or other signs of infection; sudden chest pain; arm or leg swelling; unexplained shortness of breath or difficulty breathing.
  • Advise patient, family, or caregiver to notify health care provider if rash, hives, persistent diarrhea, or excessive or unexplained tiredness develop.
  • Advise patient that drug may cause dizziness and to use caution while driving or performing other tasks requiring mental alertness or coordination until tolerance is determined.
  • Advise women that they cannot give blood while taking lenalidomide and for 4 wk after stopping therapy.
  • Advise men that they cannot donate sperm while taking lenalidomide and for 4 wk after stopping therapy.

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