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Mechlorethamine (United States: Not available) (systemic): Drug information

Mechlorethamine (United States: Not available) (systemic): Drug information
(For additional information see "Mechlorethamine (United States: Not available) (systemic): Pediatric drug information" and see "Mechlorethamine (United States: Not available) (systemic): Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
ALERT: US Boxed Warning
Experienced physician:

Mechlorethamine injection should be administered only under the supervision of a physician who is experienced in the use of cancer chemotherapeutic agents.

Extravasation:

Extravasation of the drug into subcutaneous tissues results in a painful inflammation. The area usually becomes indurated and sloughing may occur. If leakage of drug is obvious, prompt infiltration of the area with sterile isotonic sodium thiosulfate (1/6 molar) and application of an ice compress for 6 to 12 hours may minimize the local reaction. For a 1/6 molar solution of sodium thiosulfate, use 4.14 g of sodium thiosulfate per 100 mL of sterile water for injection or 2.64 g of anhydrous sodium thiosulfate per 100 mL or dilute 4 mL of sodium thiosulfate injection (10%) with 6 mL of sterile water for injection.

Hazardous agent:

Mechlorethamine is highly toxic, and both powder and solution must be handled and administered with care. Inhalation of dust or vapors and contact with skin or mucous membranes, especially those of the eyes, must be avoided. Due to the toxic properties of mechlorethamine (eg, corrosivity, carcinogenicity, mutagenicity, teratogenicity), special handling procedures should be reviewed prior to handling and followed diligently.

Brand Names: US
  • Mustargen [DSC]
Pharmacologic Category
  • Antineoplastic Agent, Alkylating Agent;
  • Antineoplastic Agent, Alkylating Agent (Nitrogen Mustard)
Dosing: Adult

Note: Mustargen has been discontinued in the United States for >1 year.

Dosage should be based on ideal dry weight (evaluate the presence of edema or ascites so that dosage is based on actual weight unaugmented by edema/ascites). Mechlorethamine is associated with a high emetic potential; antiemetics are recommended to prevent nausea and vomiting (ASCO [Hesketh 2020]; MASCC/ESMO [Roila 2016]). Dosing in the prescribing information does not reflect current clinical practice.

Hodgkin lymphoma, previously untreated

Hodgkin lymphoma, previously untreated (off-label use/dose): IV:

Stanford V regimen:

Favorable/early stage disease: 6 mg/m2 as a single dose on day 1 every 4 weeks (in combination with doxorubicin, vinblastine, vincristine, bleomycin, etoposide, prednisone, and radiation therapy) for a total of 2 cycles (Advani 2013).

Unfavorable/advanced stage disease: 6 mg/m2 as a single dose on day 1 every 4 weeks (in combination with doxorubicin, vinblastine, vincristine, bleomycin, etoposide, prednisone, and radiation therapy) for a total of 3 cycles (Bartlett 1995; Horning 2000; Horning 2002).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

The following have also been reported:

Mild-to-moderate impairment: No dosage adjustment necessary (Ecklund 2005).

Severe liver impairment: No dosage adjustment necessary; concomitant chemotherapy may require alteration until improvement in hepatic function (Ecklund 2005)

Dosing: Pediatric

(For additional information see "Mechlorethamine (United States: Not available) (systemic): Pediatric drug information")

Note: Mustargen has been discontinued in the US for >1 year.

Note: Dosing and frequency may vary by protocol and/or treatment phase; refer to specific protocol. Meclorethamine is associated with a high emetic potential; antiemetics are recommended to prevent nausea and vomiting (POGO [Dupuis 2011]).

Hodgkin lymphoma

Hodgkin lymphoma:

MOPP regimen: Note: The MOPP (with or without ABVD) regimen is generally no longer used due to improved toxicity profiles with other combination regimens used in the treatment of Hodgkin lymphoma (Kelly 2012). Children and Adolescents: IV: 6 mg/m2 on days 1 and 8 of a 28-day cycle in combination with vincristine, procarbazine, and prednisone, may or may not alternate with doxorubicin, bleomycin, vinblastine, dacarbazine (MOPP/ABVD) (Kung 2006; Longo 1986)

Stanford V regimen: Adolescents ≥16 years: IV: 6 mg/m2 as a single dose on day 1 in weeks 1, 5, and 9 (Horning 2000; Horning 2002; Metzger 2012)

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

There is no dosage adjustment provided in manufacturer's labeling.

Dosing: Hepatic Impairment: Pediatric

There is no dosage adjustment provided in manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Obesity: Adult

ASCO guidelines for appropriate chemotherapy dosing in adults with cancer with a BMI ≥30 kg/m2: In general, utilize patient’s actual body weight (full weight) for calculation of body surface area- or weight-based dosing, particularly when the intent of therapy is curative; manage regimen-related toxicities in the same manner as for patients with a BMI <30 kg/m2; if a dose reduction is utilized due to toxicity, consider resumption of full weight-based dosing with subsequent cycles, especially if cause of toxicity (eg, hepatic or renal impairment) is resolved (ASCO [Griggs 2021]). Note: The manufacturer recommends dosing be based on ideal dry body weight and the presence of edema or ascites should be considered so the dose will be based on unaugmented weight.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution Reconstituted, Injection, as hydrochloride:

Mustargen: 10 mg (1 ea [DSC])

Generic Equivalent Available: US

No

Product Availability

Mustargen has been discontinued in the United States for >1 year.

Administration: Adult

IV: Administer as a slow IV push over a few minutes into a free-flowing IV solution. Mechlorethamine is associated with a high emetic potential; antiemetics are recommended to prevent nausea and vomiting (ASCO [Hesketh 2020]; MASCC/ESMO [Roila 2016]).

Prepare immediately prior to administration.

Vesicant; ensure proper needle or catheter placement prior to and during infusion; avoid extravasation.

Extravasation management: If extravasation occurs, stop infusion immediately and disconnect (leave cannula/needle in place); gently aspirate extravasated solution (do NOT flush the line); remove needle/cannula; elevate extremity.

Sodium thiosulfate 1/6 M solution: Inject subcutaneously into extravasation area using 2 mL for each mg of mechlorethamine suspected to have extravasated (ESMO/EONS [Perez Fidalgo 2012]; Polovich 2009). Apply ice for 6 to 12 hours after sodium thiosulfate administration (Mustargen prescribing information 2013; Polovich 2009) or may apply dry cold compresses for 20 minutes 4 times daily for 1 to 2 days (ESMO/EONS [Perez Fidalgo 2012]).

Administration: Pediatric

Mechlorethamine is associated with a high emetic potential; antiemetics are recommended to prevent nausea and vomiting (POGO [Dupuis 2011]).

Parenteral: Must be prepared immediately prior to administration. Administer IV push over 1 to 5 minutes into a free-flowing IV solution. DO NOT ADMINISTER IM or SubQ.

Vesicant; ensure proper needle or catheter placement prior to and during infusion; avoid extravasation. If extravasation occurs, stop infusion immediately and disconnect (leave cannula/needle in place); gently aspirate extravasated solution (do NOT flush the line); remove needle/cannula; initiate sodium thiosulfate antidote (see Management of Drug Extravasations for more details); elevate extremity.

Hazardous Drugs Handling Considerations

Hazardous agent (NIOSH 2016 [group 1]).

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).

Use: Labeled Indications

Hodgkin lymphoma: Palliative treatment of Hodgkin lymphoma

Use: Off-Label: Adult

Hodgkin lymphoma (previously untreated)

Medication Safety Issues
High alert medication:

This medication is in a class the Institute for Safe Medication Practices (ISMP) includes among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not defined.

Cardiovascular: Local thrombophlebitis

Central nervous system: Brain disease (high dose), drowsiness, headache, lethargy, metallic taste, sedation, vertigo

Dermatologic: Alopecia, diaphoresis, erythema multiforme, maculopapular rash, skin rash

Endocrine & metabolic: Amenorrhea, hyperuricemia, oligomenorrhea

Gastrointestinal: Anorexia, diarrhea, mucositis, nausea, vomiting

Genitourinary: Inhibition of spermatogenesis

Hematologic & oncologic: Agranulocytosis, granulocytopenia (onset: 6 to 8 days; recovery: 10 to 21 days), hemolytic anemia, leukopenia, lymphocytopenia, pancytopenia, petechia, thrombocytopenia

Hepatic: Jaundice

Hypersensitivity: Anaphylaxis, hypersensitivity reaction

Infection: Herpes zoster

Neuromuscular & skeletal: Weakness

Ophthalmic: Lacrimation

Otic: Deafness, tinnitus

Miscellaneous: Fever, tissue necrosis (extravasation)

Contraindications

Hypersensitivity (prior anaphylactic reaction) to mechlorethamine or any component of the formulation; presence of known infectious diseases

Warnings/Precautions

Concerns related to adverse effects:

• Bone marrow suppression: Mechlorethamine may cause hematologic toxicity, including leukopenia, neutropenia, thrombocytopenia, anemia, and lymphopenia. The onsets for neutropenia and thrombocytopenia occur within 6 to 8 days and last for 10 to 21 days. Anemia typically has an onset within 2 weeks and is generally mild. The lymphocytopenia onset occurs within 1 day. Agranulocytopenia or hemolytic anemia may rarely occur. Severe hematologic toxicity may occur in patients with widespread disease, poor performance status, and/or those previously treated with other antineoplastic agents or radiation therapy. Bone marrow suppression may be prolonged (up to 50 days or longer); persistent pancytopenia has also been reported. Bleeding due to severe thrombocytopenia may occur. Use with caution in patients with preexisting leukopenia, thrombocytopenia, and anemia or with tumor invasion of the bone marrow; treatment response (as defined by the absence of tumor in the bone marrow) may be associated with improvement of bone marrow function. However, in nonresponders or heavily pretreated patients, hematopoietic function may be further compromised, leading to more severe (and potentially fatal) leukopenia, thrombocytopenia, and anemia. Bone marrow function should recover after mechlorethamine administration prior to initiating radiation therapy or other chemotherapy regimens.

• Extravasation: Mechlorethamine is a vesicant. [US Boxed Warning]: Extravasation results in painful inflammation with induration and sloughing. If extravasation occurs, promptly manage by infiltrating area with 1/6 molar sodium thiosulfate solution, followed by dry cold compresses for 6 to 12 hours to minimize the reaction. For a 1/6 molar solution of sodium thiosulfate, use 4.14 g of sodium thiosulfate per 100 mL of sterile water for injection or 2.64 g of anhydrous sodium thiosulfate per 100 mL or dilute 4 mL of sodium thiosulfate injection (10%) with 6 mL of sterile water for injection. Ensure proper needle or catheter placement prior to and during infusion. Avoid extravasation.

• Hypersensitivity: Hypersensitivity reactions, including anaphylaxis, have been reported.

• Immunosuppression: Mechlorethamine has immunosuppressant properties. May predispose patients to infections (bacterial, viral, or fungal).

• Secondary malignancies: Alkylating agents, including mechlorethamine, are associated with an increased incidence of secondary malignancies; concurrent radiation therapy or combination chemotherapy may increase the risk.

• Tumor lysis syndrome: Hyperuricemia may occur, especially with lymphomas; ensure adequate hydration; consider antihyperuricemic therapy if appropriate.

Disease-related concerns:

• Amyloidosis: Nitrogen mustards may contribute to extensive/rapid development of amyloidosis. Mechlorethamine should only be used if foci of suppurative inflammation (acute and chronic) are absent.

• Nonresponding tumors: Bone and nervous system tumors typically respond poorly to mechlorethamine. The routine use of mechlorethamine in widely disseminated tumors is discouraged.

Special handling:

• Hazardous agent: [US Boxed Warning]: Mechlorethamine is a highly toxic nitrogen mustard; avoid inhalation of vapors or dust; avoid dust or vapor contact with skin or eyes; review and follow special handling procedures. If accidental skin exposure occurs, wash/irrigate thoroughly with water for at least 15 minutes, followed by 2% sodium thiosulfate solution; remove and destroy any contaminated clothing. If exposure to eye(s) occurs, promptly irrigate for at least 15 minutes with copious amounts of water, normal saline, or balanced salt ophthalmic irrigating solution; obtain ophthalmology consultation. The manufacturer recommends neutralizing remaining unused mechlorethamine, empty or partial vials, gloves, tubing, glassware, etc., after mechlorethamine administration; soak in an aqueous solution containing equal volumes of sodium thiosulfate (5%) and sodium bicarbonate (5%) for 45 minutes; rinse with water; dispose of properly.

Other warnings/precautions:

• Topical application: A gel formulation is commercially approved for topical treatment of cutaneous T-cell lymphoma (mycosis fungoides-type); refer to Mechlorethamine (Topical) monograph.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

5-Aminosalicylic Acid Derivatives: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy

Abrocitinib: May enhance the immunosuppressive effect of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid combination

Baricitinib: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Baricitinib. Risk X: Avoid combination

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

BCG Products: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the adverse/toxic effect of BCG Products. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of BCG Products. Risk X: Avoid combination

Brincidofovir: Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Brincidofovir. Risk C: Monitor therapy

Chloramphenicol (Ophthalmic): May enhance the adverse/toxic effect of Myelosuppressive Agents. Risk C: Monitor therapy

Cladribine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk X: Avoid combination

Cladribine: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Cladribine. Risk X: Avoid combination

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

Coccidioides immitis Skin Test: Immunosuppressants (Cytotoxic Chemotherapy) may diminish the diagnostic effect of Coccidioides immitis Skin Test. Management: Consider discontinuing cytotoxic chemotherapy several weeks prior to coccidioides immitis skin antigen testing to increase the likelihood of accurate diagnostic results. Risk D: Consider therapy modification

COVID-19 Vaccine (Adenovirus Vector): Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of COVID-19 Vaccine (Adenovirus Vector). Management: Administer a 2nd dose using an mRNA COVID-19 vaccine (at least 4 weeks after the primary vaccine dose) and a bivalent booster dose (at least 2 months after the additional mRNA dose or any other boosters). Risk D: Consider therapy modification

COVID-19 Vaccine (Inactivated Virus): Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of COVID-19 Vaccine (Inactivated Virus). Risk C: Monitor therapy

COVID-19 Vaccine (mRNA): Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of COVID-19 Vaccine (mRNA). Management: Give a 3-dose primary series for all patients aged 6 months and older taking immunosuppressive medications or therapies. Booster doses are recommended for certain age groups. See CDC guidance for details. Risk D: Consider therapy modification

COVID-19 Vaccine (Subunit): Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of COVID-19 Vaccine (Subunit). Risk C: Monitor therapy

COVID-19 Vaccine (Virus-like Particles): Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of COVID-19 Vaccine (Virus-like Particles). Risk C: Monitor therapy

Deferiprone: Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Risk D: Consider therapy modification

Dengue Tetravalent Vaccine (Live): Immunosuppressants (Cytotoxic Chemotherapy) may enhance the adverse/toxic effect of Dengue Tetravalent Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Dengue Tetravalent Vaccine (Live). Risk X: Avoid combination

Denosumab: May enhance the immunosuppressive effect of Immunosuppressants (Cytotoxic Chemotherapy). Management: Consider the risk of serious infections versus the potential benefits of coadministration of denosumab and cytotoxic chemotherapy. If combined, monitor patients for signs/symptoms of serious infections. Risk D: Consider therapy modification

Deucravacitinib: May enhance the immunosuppressive effect of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid combination

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

Fexinidazole: Myelosuppressive Agents may enhance the myelosuppressive effect of Fexinidazole. Risk X: Avoid combination

Filgotinib: May enhance the immunosuppressive effect of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid combination

Inebilizumab: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Inebilizumab. Risk C: Monitor therapy

Influenza Virus Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Influenza Virus Vaccines. Management: Administer influenza vaccines at least 2 weeks prior to initiating chemotherapy if possible. If vaccination occurs less than 2 weeks prior to or during chemotherapy, revaccinate at least 3 months after therapy discontinued if immune competence restored. Risk D: Consider therapy modification

Leflunomide: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Leflunomide. Management: Increase the frequency of chronic monitoring of platelet, white blood cell count, and hemoglobin or hematocrit to monthly, instead of every 6 to 8 weeks, if leflunomide is coadministered with immunosuppressive agents, such as cytotoxic chemotherapy. Risk D: Consider therapy modification

Lenograstim: Antineoplastic Agents may diminish the therapeutic effect of Lenograstim. Management: Avoid the use of lenograstim 24 hours before until 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Risk D: Consider therapy modification

Lipegfilgrastim: Antineoplastic Agents may diminish the therapeutic effect of Lipegfilgrastim. Management: Avoid concomitant use of lipegfilgrastim and myelosuppressive cytotoxic chemotherapy. Lipegfilgrastim should be administered at least 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Risk D: Consider therapy modification

Natalizumab: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Natalizumab. Risk X: Avoid combination

Ocrelizumab: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Ocrelizumab. Risk C: Monitor therapy

Ofatumumab: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Ofatumumab. Risk C: Monitor therapy

Olaparib: Myelosuppressive Agents may enhance the myelosuppressive effect of Olaparib. Risk C: Monitor therapy

Palifermin: May enhance the adverse/toxic effect of Antineoplastic Agents. Specifically, the duration and severity of oral mucositis may be increased. Management: Do not administer palifermin within 24 hours before, during infusion of, or within 24 hours after administration of myelotoxic chemotherapy. Risk D: Consider therapy modification

Pidotimod: Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Pidotimod. Risk C: Monitor therapy

Pimecrolimus: May enhance the immunosuppressive effect of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid combination

Pneumococcal Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Pneumococcal Vaccines. Risk C: Monitor therapy

Poliovirus Vaccine (Live/Trivalent/Oral): Immunosuppressants (Cytotoxic Chemotherapy) may enhance the adverse/toxic effect of Poliovirus Vaccine (Live/Trivalent/Oral). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Poliovirus Vaccine (Live/Trivalent/Oral). Risk X: Avoid combination

Polymethylmethacrylate: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the potential for allergic or hypersensitivity reactions to Polymethylmethacrylate. Management: Use caution when considering use of bovine collagen-containing implants such as the polymethylmethacrylate-based Bellafill brand implant in patients who are receiving immunosuppressants. Consider use of additional skin tests prior to administration. Risk D: Consider therapy modification

Promazine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy

Rabies Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Rabies Vaccine. Management: Complete rabies vaccination at least 2 weeks before initiation of immunosuppressant therapy if possible. If combined, check for rabies antibody titers, and if vaccination is for post exposure prophylaxis, administer a 5th dose of the vaccine. Risk D: Consider therapy modification

Ropeginterferon Alfa-2b: Myelosuppressive Agents may enhance the myelosuppressive effect of Ropeginterferon Alfa-2b. Management: Avoid coadministration of ropeginterferon alfa-2b and other myelosuppressive agents. If this combination cannot be avoided, monitor patients for excessive myelosuppressive effects. Risk D: Consider therapy modification

Rubella- or Varicella-Containing Live Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the adverse/toxic effect of Rubella- or Varicella-Containing Live Vaccines. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Rubella- or Varicella-Containing Live Vaccines. Risk X: Avoid combination

Ruxolitinib (Topical): Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Ruxolitinib (Topical). Risk X: Avoid combination

Sipuleucel-T: Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Sipuleucel-T. Management: Consider reducing the dose or discontinuing the use of immunosuppressants, such as cytotoxic chemotherapy, prior to initiating sipuleucel-T therapy. Risk D: Consider therapy modification

Sphingosine 1-Phosphate (S1P) Receptor Modulator: May enhance the immunosuppressive effect of Immunosuppressants (Cytotoxic Chemotherapy). Risk C: Monitor therapy

Tacrolimus (Topical): Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Tacrolimus (Topical). Risk X: Avoid combination

Talimogene Laherparepvec: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the adverse/toxic effect of Talimogene Laherparepvec. Specifically, the risk of infection from the live, attenuated herpes simplex virus contained in talimogene laherparepvec may be increased. Risk X: Avoid combination

Tertomotide: Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Tertomotide. Risk X: Avoid combination

Tofacitinib: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Tofacitinib. Risk X: Avoid combination

Typhoid Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the adverse/toxic effect of Typhoid Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Typhoid Vaccine. Risk X: Avoid combination

Upadacitinib: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the immunosuppressive effect of Upadacitinib. Risk X: Avoid combination

Vaccines (Inactivated/Non-Replicating): Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Vaccines (Inactivated/Non-Replicating). Management: Give inactivated vaccines at least 2 weeks prior to initiation of chemotherapy when possible. Patients vaccinated less than 14 days before initiating or during chemotherapy should be revaccinated at least 3 months after therapy is complete. Risk D: Consider therapy modification

Vaccines (Live): Immunosuppressants (Cytotoxic Chemotherapy) may enhance the adverse/toxic effect of Vaccines (Live). Specifically, the risk of vaccine-associated infection may be increased. Vaccines (Live) may diminish the therapeutic effect of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid combination

Yellow Fever Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may enhance the adverse/toxic effect of Yellow Fever Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may diminish the therapeutic effect of Yellow Fever Vaccine. Risk X: Avoid combination

Reproductive Considerations

Females of reproductive potential are advised not to become pregnant during mechlorethamine treatment.

Delayed menses, oligomenorrhea, or temporary or permanent amenorrhea may be observed in female patients treated with mechlorethamine. Impaired spermatogenesis, azoospermia, and total germinal aplasia may occur in male patients treated with mechlorethamine, particularly when used in combination with other chemotherapy agents.

Pregnancy Considerations

[US Boxed Warning]: Mechlorethamine is highly toxic, and both powder and solution must be handled and administered with care. Inhalation of dust or vapors and contact with skin or mucous membranes, especially those of the eyes, must be avoided. Avoid exposure during pregnancy. Due to the toxic properties of mechlorethamine (eg, teratogenicity), special handling procedures should be reviewed prior to handling and followed diligently.

Mechlorethamine may cause fetal harm if administered to a pregnant female.

Breastfeeding Considerations

It is not known if mechlorethamine is present in human breast milk. Due to the potential for serious adverse reactions in the breastfeeding infant, a decision should be made to discontinue mechlorethamine or to discontinue breastfeeding, taking into account the importance of treatment to the mother.

Monitoring Parameters

CBC with differential and platelet count; renal and hepatic function. Monitor for signs/symptoms of hypersensitivity reactions, tumor lysis syndrome, secondary malignancies, and infection. Monitor infusion site for extravasation.

The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.

Mechanism of Action

Mechlorethamine is a bifunctional alkylating agent that inhibits DNA and RNA synthesis via formation of carbonium ions; produces interstrand and intrastrand cross-links in DNA resulting in miscoding, breakage, and failure of replication. Although not cell phase-specific per se, mechlorethamine effect is most pronounced in the S phase, and cell proliferation is arrested in the G2 phase.

Pharmacokinetics

Metabolism: Rapid hydrolysis in the plasma to active metabolites (Perry 2012)

Half-life elimination: 15 to 20 minutes (Perry 2012)

Pricing: US

Solution (reconstituted) (Mustargen Injection)

10 mg (per each): $371.65

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Caryolysine (FR, GR);
  • Ledaga (IL);
  • Mustargen (BB, IL)


For country code abbreviations (show table)
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