pharmacopeia
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/api/v1/drug/mechlorethamine

Mechanism of action

Sourced from openFDA

Mechlorethamine, also known as nitrogen mustard, is an alkylating agent which inhibits rapidly proliferating cells.

Indications

Sourced from openFDA
  • VALCHLOR is indicated for the topical treatment of Stage IA and IB mycosis fungoides-type cutaneous T-cell lymphoma in patients who have received prior skin-directed therapy. VALCHLOR is an alkylating drug indicated for the topical treatment of Stage IA and IB mycosis fungoides-type cutaneous T-cell lymphoma in patients who have received prior skin-directed therapy ( 1 ).ICD-10: C85.90

Contraindications

Sourced from openFDA
  • The use of VALCHLOR is contraindicated in patients with known severe hypersensitivity to mechlorethamine. Hypersensitivity reactions, including anaphylaxis, have occurred with topical formulations of mechlorethamine.contraindicated

Dosage & administration

Sourced from openFDA

For topical dermatological use only ( 2.1 ). Apply a thin film once daily to affected areas of the skin ( 2.1 , 2.2 ). 2.1 Dosing and Dose Modification For Topical Dermatological Use Only Apply a thin film of VALCHLOR gel once daily to affected areas of the skin. Stop treatment with VALCHLOR for any grade of skin ulceration, blistering, or moderately-severe or severe dermatitis (i.e., marked skin redness with edema) [ see Warnings and Precautions ( 5.3 ) ]. Upon improvement, treatment with VALCHLOR can be restarted at a reduced frequency of once every 3 days. If reintroduction of treatment is tolerated for at least one week, the frequency of application can be increased to every other day for at least one week and then to once daily application if tolerated. 2.2 Application Instructions VALCHLOR is a cytotoxic drug. Follow applicable special handling and disposal procedures. 1 Patients must wash hands thoroughly with soap and water after handling or applying VALCHLOR. Caregivers must wear disposable nitrile gloves when applying VALCHLOR to patients and wash hands thoroughly with soap and water after removal of gloves. If there is accidental skin exposure to VALCHLOR, caregivers must immediately wash exposed areas thoroughly with soap and water for at least 15 minutes and remove contaminated clothing [ see Warnings and Precautions ( 5.2 ) ]. Patients or caregivers should follow these instructions when applying VALCHLOR: Apply immediately or within 30 minutes after removal from the refrigerator. Return VALCHLOR to the refrigerator immediately after each use.

Warnings & precautions

Sourced from openFDA

Mucosal or eye injury: VALCHLOR exposure to mucous membranes, especially of the eyes, can cause mucosal injury which may be severe. Eye injury may lead to blindness. Immediately irrigate for at least 15 minutes followed by immediate medical consultation ( 5.1 ). Secondary exposure to VALCHLOR: individuals other than the patient must avoid skin contact with VALCHLOR ( 2.2 , 5.2 ). Dermatitis: Monitor patients for redness, swelling, inflammation, itchiness, blisters, ulceration, and secondary skin infections. Stop treatment or reduce dose frequency ( 2.1 , 5.3 ). Non-melanoma skin cancer: Monitor patients during and after treatment ( 5.4 ). Embryo-fetal toxicity: May cause fetal harm ( 5.5 ). Flammable gel: VALCHLOR is an alcohol-based gel. Avoid fire, flame, and smoking until the gel has dried ( 2.2 , 5.6 ). 5.1 Mucosal or Eye Injury Exposure of the eyes to mechlorethamine causes pain, burns, inflammation, photophobia, and blurred vision. Blindness and severe irreversible anterior eye injury may occur. Advise patients that if eye exposure occurs, (1) immediately irrigate for at least 15 minutes with copious amounts of water, normal saline, or a balanced salt ophthalmic irrigating solution and (2) obtain immediate medical care (including ophthalmologic consultation). Exposure of mucous membranes such as the oral mucosa or nasal mucosa causes pain, redness, and ulceration, which may be severe. Should mucosal contact occur, immediately irrigate for at least 15 minutes with copious amounts of water, followed by immediate medical consultation.

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are discussed in greater detail in other sections of the prescribing information: Mucosal or eye injury [ see Warnings and Precautions ( 5.1 ) ] Secondary exposure to VALCHLOR [ see Warnings and Precautions ( 5.2 ) ] Dermatitis [ see Warnings and Precautions ( 5.3 ) ] Non-melanoma skin cancer [ see Warnings and Precautions ( 5.4 ) ] The most common adverse reactions (≥5%) are dermatitis, pruritus, bacterial skin infection, skin ulceration or blistering, and hyperpigmentation ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Helsinn Therapeutics (U.S.), Inc., at 1-855-482-5245 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. In a randomized, observer-blinded, controlled trial, VALCHLOR 0.016% (equivalent to 0.02% mechlorethamine HCl) was compared to an Aquaphor ® -based mechlorethamine HCl 0.02% ointment (Comparator) [ see Clinical Studies ( 14 ) ]. The maximum duration of treatment was 12 months. Sixty-three percent (63%) of patients in the VALCHLOR arm and 67% in the comparator arm completed 12 months of treatment. The body system associated with the most frequent adverse reactions was skin and subcutaneous tissue disorders.

Use in specific populations

Sourced from openFDA

Lactation: Advise not to breastfeed ( 8.2 ). 8.1 Pregnancy Risk Summary Based on case reports in humans, findings in animal reproduction studies, its mechanism of action, and genotoxicity findings, mechlorethamine may cause fetal harm. Available published case reports in pregnant women receiving intravenous mechlorethamine demonstrate that mechlorethamine can cause major birth defects when a pregnant woman is systemically exposed. In animal reproduction studies, subcutaneous administration of mechlorethamine to pregnant rats and ferrets during organogenesis resulted in embryo‐fetal mortality, alterations to growth, and structural abnormalities. Based on limited available data with VALCHLOR use in pregnant women, if VALCHLOR is used during pregnancy or if the patient becomes pregnant while taking this drug, patient should be advised of the potential risk to the fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Human Data The limited available data with VALCHLOR use in pregnant women does not show evidence of congenital malformation in newborns.

Pharmacokinetics

Sourced from openFDA
Metabolism
Systemic exposure was undetectable after topical administration of VALCHLOR to patients. Blood samples were analyzed from 16 and 15 patients following treatment with VALCHLOR (mechlorethamine gel 0.016%) and an identical formulation consisting of mechlorethamine 0.032% w/w, respectively.

Approval history

Sourced from openFDA
  • Aug 23, 2013NDANDA202317Helsinn

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
2,237 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Pruritus32114%
  2. 2Application Site Pruritus22410%
  3. 3Application Site Erythema2209.8%
  4. 4Application Site Pain2179.7%
  5. 5Erythema2109.4%
  6. 6Condition Aggravated1938.6%
  7. 7Off Label Use1767.9%
  8. 8Skin Discolouration1476.6%
  9. 9Rash1325.9%
  10. 10Skin Irritation1125.0%
  11. 11Blister1074.8%
  12. 12Application Site Discolouration1024.6%
  13. 13Application Site Irritation1014.5%
  14. 14Disease Progression994.4%
  15. 15Death984.4%

Literature

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Recent PubMed references pinned to Mechlorethamine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 4,977 ClinicalTrials.gov registrations naming Mechlorethamine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Mechlorethamine work?
Mechlorethamine, also known as nitrogen mustard, is an alkylating agent which inhibits rapidly proliferating cells.
What is Mechlorethamine used for?
According to FDA labeling, Mechlorethamine carries indications including: VALCHLOR is indicated for the topical treatment of Stage IA and IB mycosis fungoides-type cutaneous T-cell lymphoma in patients who have received prior skin-directed therapy. VALCHLOR is an alkylating drug indicated for the topical treatment of Stage IA and IB mycosis fungoides-type cutaneous T-cell lymphoma in patients who have received prior skin-directed therapy ( 1 ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Mechlorethamine?
Mechlorethamine is classified as Nitrogen mustard analogues, Alkylating Drug, Alkylating Activity, Decreased DNA Integrity, Decreased DNA Replication.
What are the brand names for Mechlorethamine?
Mechlorethamine is marketed under brand names including Valchlor.
What are the contraindications for Mechlorethamine?
Mechlorethamine labeling lists contraindications including: The use of VALCHLOR is contraindicated in patients with known severe hypersensitivity to mechlorethamine. Hypersensitivity reactions, including anaphylaxis, have occurred with topical formulations of mechlorethamine.. Always consult the full prescribing information and a clinician.
Note. Data for mechlorethamine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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