Home

helps physicians and healthcare professionals

Erectile Dysfunction

helps physicians and healthcare professionals

Doctor123.org

helps physicians and healthcare professionals

RomiDEPsin


General


Pronunciation

(roe mi DEP sin)


Brand Names: U.S.

  • Istodax

Indications


Use: Labeled Indications

Cutaneous T-cell lymphoma: Treatment of cutaneous T-cell lymphoma (CTCL) in patients who have received at least one prior systemic therapy

Peripheral T-cell lymphoma: Treatment of peripheral T-cell lymphoma (PTCL) in patients who have received at least one prior therapy


Contraindications


There are no contraindications listed in the manufacturer 's labeling.


Dosing and Administration


Dosing: Adult

Note: Romidepsin is associated with a moderate emetic potential; antiemetics are recommended to prevent nausea and vomiting (MASCC 2016).

Cutaneous T-cell lymphoma: IV: 14 mg/m2 days 1, 8, and 15 of a 28-day treatment cycle; repeat cycle as long as benefit continues and treatment is tolerated.

Peripheral T-cell lymphoma: IV: 14 mg/m2 days 1, 8, and 15 of a 28-day treatment cycle; repeat cycle as long as benefit continues and treatment is tolerated.


Dosing: Geriatric

Refer to adult dosing.


Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer 's labeling (has not been studied). However, dosage adjustment is not likely necessary since pharmacokinetics are unaffected by renal impairment. Use with caution in patients with end-stage renal disease (has not been studied).


Dosing: Hepatic Impairment

Mild impairment: There are no dosage adjustments provided in the manufacturer 's labeling. However, mild hepatic impairment does not significantly influence the pharmacokinetics of romidepsin.

Moderate or severe impairment: There are no dosage adjustments provided in the manufacturer 's labeling. Use with caution.


Reconstitution

Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]). Reconstitute each vial of romidepsin with 2.2 mL of supplied diluent to a reconstituted concentration of 5 mg/mL (both the drug and diluent vials contain overfill to ensure the appropriate volume can be withdrawn); swirl until dissolved. The reconstituted vial will contain a deliverable volume of 2 mL of product. Further dilute in 500 mL normal saline; compatible with polyvinyl chloride (PVC), ethylene vinyl acetate (EVA), polyethylene (PE) and glass infusion containers.


Administration

Romidepsin is associated with a moderate emetic potential; antiemetics are recommended to prevent nausea and vomiting (MASCC 2016). Antiemetics were used in clinical trials to prevent nausea and vomiting (Piekarz 2009; Piekarz 2011).

Infuse over 4 hours.

Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]).


Dietary Considerations

Avoid grapefruit juice.


Storage

Store intact vials at room temperature of 20 ‚ °C to 25 ‚ °C (68 ‚ °F to 77 ‚ °F); excursions are permitted between 15 ‚ °C and 30 ‚ °C (59 ‚ °F and 86 ‚ °F). The reconstituted solution is stable for 8 hours at room temperature. Solutions diluted for infusion in NS are stable for 24 hours at room temperature; however, the manufacturer recommends use as soon as possible after dilution.


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous:

Istodax: 10 mg (1 ea) [contains alcohol, usp, propylene glycol]


Compatibility

Stable in NS.


Drug Interactions

BCG (Intravesical): Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG (Intravesical): Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

CloZAPine: Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased. Monitor therapy

Coccidioides immitis Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test. Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of RomiDEPsin. Avoid combination

CYP3A4 Inhibitors (Strong): May increase the serum concentration of RomiDEPsin. Monitor therapy

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Deferiprone: Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Avoid combination

Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. Monitor therapy

Dexamethasone (Systemic): May decrease the serum concentration of RomiDEPsin. Avoid combination

Dipyrone: May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased Avoid combination

Echinacea: May diminish the therapeutic effect of Immunosuppressants. Consider therapy modification

Fingolimod: Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections). Consider therapy modification

Highest Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification

Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Consider therapy modification

MiFEPRIStone: May enhance the QTc-prolonging effect of QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying). Management: Though the drugs listed here have uncertain QT-prolonging effects, they all have some possible association with QT prolongation and should generally be avoided when possible. Consider therapy modification

Moderate Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Monitor therapy

Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Avoid combination

Nivolumab: Immunosuppressants may diminish the therapeutic effect of Nivolumab. Consider therapy modification

Osimertinib: May increase the serum concentration of CYP3A4 Substrates. Osimertinib may decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Ranolazine: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

RifAMPin: May increase the serum concentration of RomiDEPsin. Avoid combination

Roflumilast: May enhance the immunosuppressive effect of Immunosuppressants. Consider therapy modification

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Monitor therapy

St Johns Wort: May decrease the serum concentration of RomiDEPsin. Avoid combination

Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Tofacitinib: Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants. Avoid combination

Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Monitor therapy

Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation. Consider therapy modification

Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Management: Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants. Avoid combination

Warfarin: RomiDEPsin may enhance the anticoagulant effect of Warfarin. Monitor therapy


Monitoring Parameters

Serum electrolytes (baseline and periodic; especially potassium and magnesium); CBC with differential and platelets, ECG (baseline and periodic; in patients with significant cardiovascular disease, congenital long QT syndrome, and in patients taking QT-prolonging medications); signs/symptoms of infection or tumor lysis syndrome


Adverse Reactions


>10%:

Cardiovascular: ST-T wave changes (2% to 63%), hypotension (7% to 23%)

Central nervous system: Fatigue (53% to 77%), fever (20% to 47%), headache (15% to 34%), chills (11% to 17%)

Dermatologic: Pruritus (7% to 31%), dermatitis/exfoliative dermatitis (4% to 27%)

Endocrine & metabolic: Hypocalcemia (4% to 52%), hyperglycemia (2% to 51%), hypoalbuminemia (3% to 48%), hyperuricemia ( ≤33%), hypomagnesemia (22% to 28%), hypermagnesemia ( ≤27%), hypophosphatemia ( ≤27%), hypokalemia (6% to 20%), hyponatremia ( ≤20%)

Gastrointestinal: Nausea (56% to 86%; grades 3/4: 2% to 6%), anorexia (23% to 54%), vomiting (34% to 52%; grades 3/4: ≤10%), taste alteration (15% to 40%), constipation (12% to 40%), diarrhea (20% to 36%), weight loss (10% to 15%), abdominal pain (13% to 14%)

Hematologic: Anemia (19% to 72%; grades 3/4: 3% to 28%), thrombocytopenia (17% to 72%; grades 3/4: ≤36%), neutropenia (11% to 66%; grades 3/4: 4% to 47%), lymphopenia (4% to 57%; grades 3/4: ≤37%), leukopenia (4% to 55%; grades 3/4: ≤45%)

Hepatic: AST increased (3% to 28%), ALT increased (3% to 22%)

Neuromuscular & skeletal: Weakness (53% to 77%)

Respiratory: Cough (18% to 21%), dyspnea (13% to 21%)

Miscellaneous: Infection (46% to 54%; grades 3/4: 11% to 33%)

1% to 10%:

Cardiovascular: Peripheral edema (6% to 10%), tachycardia ( ≤10%), chest pain, DVT, edema, QT prolongation, supraventricular arrhythmia, syncope, ventricular arrhythmia

Dermatologic: Cellulitis

Endocrine & metabolic: Dehydration

Gastrointestinal: Stomatitis (6% to 10%)

Hematologic: Neutropenic fever

Hepatic: Hyperbilirubinemia

Respiratory: Hypoxia, pneumonia, pneumonitis, pulmonary embolism

Miscellaneous: Central line infection, hypersensitivity, sepsis, tumor lysis syndrome (1% to 2%)

<1% (Limited to important or life-threatening): Acute renal failure, acute respiratory distress syndrome, atrial fibrillation, bacteremia, candida infection, cardiopulmonary failure, cardiogenic shock, Epstein-Barr virus reactivation, multiorgan failure, septic shock


Warnings/Precautions


Concerns related to adverse effects:

- Bone marrow suppression: Anemia, leukopenia, neutropenia, lymphopenia and thrombocytopenia may occur. May require dosage modification. Monitor blood counts during treatment.

- Gastrointestinal toxicity: Romidepsin is associated with a moderate emetic potential; antiemetics are recommended to prevent nausea and vomiting (MASCC 2016).

- Infection: Serious infections (occasionally fatal), including pneumonia, sepsis, and viral reactivation (eg, Epstein Barr and hepatitis B) have occurred during or within 30 days of treatment. Monitor patients with a history of hepatitis B infections closely for viral reactivation; consider antiviral prophylaxis. Epstein Barr reactivation leading to liver failure has also been reported, with ganciclovir antiviral prophylaxis failure in one case. The risk of life-threatening infection may be increased in patients who have received prior treatment with antilymphocytic monoclonal antibodies or who have disease involvement in the bone marrow.

- QTc prolongation/ECG changes: QTc prolongation has been observed; use caution in patients with a history of QTc prolongation, congenital long QT syndrome, with medications known to prolong the QT interval, or with pre-existing cardiac disease. Obtain baseline and periodic ECG (12-lead); monitor and correct electrolyte (potassium, magnesium, and calcium) abnormalities prior to and during treatment. T-wave and ST-segment changes have also been reported.

- Tumor lysis syndrome: Tumor lysis syndrome (TLS) has been observed; closely monitor patients with advanced disease and/or with a high tumor burden (risk of TLS is higher). If TLS occurs, initiate appropriate treatment.

Disease-related concerns:

- Hepatic impairment: Mild hepatic impairment does not significantly influence the pharmacokinetics of romidepsin (based on pharmacokinetic analysis). The effect of moderate or severe impairment is unknown; use with caution.

- Renal impairment: The pharmacokinetics of romidepsin are unaffected by mild, moderate or severe renal impairment (based on pharmacokinetic analysis). Use with caution in patients with end-stage renal disease (has not been studied).

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special handling:

- Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]).


Pregnancy Risk Factor

D


Pregnancy Considerations

Adverse events were observed in animal reproduction studies. Based on the mechanism of action, romidepsin may cause fetal harm if administered during pregnancy.


Actions


Pharmacology

Histone deacetylase inhibitor; catalyzes acetyl group removal from protein lysine residues (including histone and transcription factors). Inhibition of histone deacetylase results in accumulation of acetyl groups, leading to alterations in chromatin structure and transcription factor activation causing termination of cell growth (induces arrest in cell cycle at G1 and G2/M phases) leading to cell death.


Metabolism

Hepatic, primarily via CYP3A4, minor metabolism from CYP3A5, 1A1, 2B6 and 2C19


Half-Life Elimination

~3 hours


Protein Binding

92% to 94%; primarily toα1-acid glycoprotein


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience headache, constipation, diarrhea, lack of appetite, abdominal pain, weight loss, nausea, vomiting, change in taste, or mouth sores. Have patient report immediately to prescriber signs of infection, signs of low magnesium (mood changes; muscle pain or weakness; muscle cramps or spasms; seizures; tremors; lack of appetite; severe nausea or vomiting; or an abnormal heartbeat), signs of low potassium (muscle pain or weakness, muscle cramps, or an abnormal heartbeat), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), shortness of breath, coughing up blood, angina, tachycardia, arrhythmia, severe dizziness, passing out, bruising, bleeding, severe loss of strength and energy, urinary retention, change in amount of urine passed, or signs of tumor lysis syndrome (fast heartbeat or abnormal heartbeat; any passing out; trouble passing urine; muscle weakness or cramps; nausea, vomiting, diarrhea or lack of appetite; or feeling sluggish) (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Copyright © 2016 - 2017
Doctor123.org | Disclaimer