For US Healthcare Professionals Only

VALCHLOR^® (mechlorethamine) gel is an alkylating drug indicated for the topical treatment of Stage IA and IB mycosis fungoides–type cutaneous T-cell lymphoma (MF-CTCL) in patients who have received prior skin-directed therapy

How VALCHLOR works:
Mechanism of action and formulation

Mechlorethamine is an alkylating agent that inhibits rapidly proliferating cells¹

Induces double-stranded DNA breaks which initiate apoptosis²
Increases expression of CASP3 gene in malignant T cells which facilitates apoptosis²
Demonstrates down regulation of several important DNA repair pathways in malignant T cells from mycosis fungoides–type cutaneous T-cell lymphoma (MF-CTCL) lesions²

MF-CTCL is mediated by neoplastic malignant Th2 helper T cells that become resident and accumulate in the skin, exhibiting a pattern of abnormal behaviors: uncontrolled proliferation and epidermotropism.^3-9

Upon application, mechlorethamine enters the skin and is taken up by cells in the epidermis and dermis.^1,2

Mechlorethamine is a bifunctional alkylating agent that inhibits rapidly proliferating neoplastic T cells through its cytotoxic effects.¹⁰

This leads to the apoptosis of rapidly dividing malignant T cells.²

Treatment with mechlorethamine gel may have an effect on the typical manifestations of Stage IA/IB MF-CTCL, including patches and plaques...¹

...leading to symptom reduction in many cases.^1*

*VALCHLOR (n=119) was assessed in a 12-month randomized, multicenter, observer-blinded, nonInferiority study trial (N=260) vs Aquaphor^®-based mechlorethamine HCI 0.02%. Primary endpoint: response by CAILS (Composite Assessment Index Lesion Severity) score (combined scores for erythema, scaling, plaque elevation, and surface area). CAILS ORR: 60% (PR 45% + CR 14%). VALCHLOR nonInferiority demonstrated by the rate ratio of 1.24 (95% CI, 0.98, 1.58). ORR (overall response rate) = PR (partial response) + CR (complete response, defined as score of 0).¹

Click below to watch a video on the mechanism of action

Active ingredient

Mechlorethamine^1,2

Inhibits rapidly proliferating cells and induces apoptosis of malignant T cells

Other ingredients

Solvents and cosolvents^1,11

Diethylene glycol monoethyl ether + propylene glycol + isopropyl alcohol + glycerin
Deliver mechlorethamine to the epidermal and dermal layers of the skin

Hydroxypropylcellulose^1,12

Creates a semisolid-like gel viscosity to keep mechlorethamine in sustained contact with the affected area

Formulation

Non-greasy gel^1,10,13

Lack of water in formulation provides greater stability
VALCHLOR is stable
- 4 years in the freezer at -5ºF to -13ºF (-15ºC to -25ºC)
- 90 days with refrigeration and with daily excursion from refrigeration no longer than 1 hour

Manufacturing process

Consistent and predictable¹⁰

Manufacturing specifications ensure consistent quality and concentration from batch to batch

Homogenous¹⁰

The manufacturing process completely dissolves mechlorethamine into the formulation to ensure homogenous distribution throughout the gel

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Important Safety Information

Contraindications

VALCHLOR is contraindicated in patients with known severe hypersensitivity to mechlorethamine. Hypersensitivity reactions, including anaphylaxis, have occurred with topical formulations of mechlorethamine.

Warnings And Precautions

Mucosal or eye injury: Exposure of mucous membranes to mechlorethamine such as the oral mucosa or nasal mucosa causes pain, redness, and ulceration, which may be severe. Exposure of the eyes causes pain, burns, inflammation, photophobia, and blurred vision. Blindness and severe irreversible anterior eye injury may occur. Should eye exposure or mucosal contact occur, immediately irrigate for at least 15 minutes with copious amounts of water, followed by immediate medical consultation
Secondary exposure: Avoid direct skin contact with VALCHLOR in individuals other than the patients due to risk of dermatitis, mucosal injury, and secondary cancers
Dermatitis: Dermatitis may be moderately severe or severe. Monitor patients for redness, swelling, inflammation, itchiness, blisters, ulceration, and secondary skin infections. Stop treatment with VALCHLOR or reduce dose frequency
Non-melanoma skin cancer: Monitor patients during and after treatment with VALCHLOR
Embryo-fetal toxicity: May cause fetal harm. Women should avoid becoming pregnant while using VALCHLOR due to the potential hazard to the fetus. For nursing mothers, do not breastfeed during treatment with VALCHLOR
Flammable gel: VALCHLOR is an alcohol-based gel. Avoid fire, flame, and smoking until the gel has dried

Adverse Reactions

The most common adverse reactions (≥5%) were dermatitis (56%), pruritus (20%), bacterial skin infection (11%), skin ulceration or blistering (6%), and hyperpigmentation (5%). These reactions may be moderately severe or severe. Elderly patients aged 65 and older may be more susceptible. Depending on severity, treatment reduction, suspension, or discontinuation may be required.

Use In Specific Populations

Contraception: Females who are able to become pregnant, and males with female partners who are able to become pregnant, should use a barrier method of contraception to avoid direct exposure of reproductive organs to VALCHLOR
Infertility: The reproductive effects of VALCHLOR have not been studied: however systemically administered mechlorethamine may impair fertility. The reversibility of the effect on fertility is unknown.

Dosing and Application

VALCHLOR is for topical dermatologic use only. Apply a thin film of gel once daily to affected areas of the skin. VALCHLOR is a cytotoxic drug and special handling and disposal procedures should be followed during use. Caregivers must wear disposable nitrile gloves when applying VALCHLOR. Patients and caregivers must thoroughly wash hands after handling or applying VALCHLOR.

To report SUSPECTED ADVERSE REACTIONS, contact Helsinn Therapeutics (U.S.), Inc. at 1-855-482-5245 or FDA at 1-800-FDA-1088 or visit www.fda.gov/medwatch.

Please see the VALCHLOR full Prescribing Information and Medication Guide (EN/ES).

References:

VALCHLOR [package insert]. Iselin, NJ: Helsinn Therapeutics US, Inc.; January 2020.
Chang YT et al. JID Innov. 2022;2(1):100069.
Kim EJ et al. J Clin Invest. 2005;115(4):798-812.
Girardi M et al. N Engl J Med. 2004;350(19):1978-1988.
McGirt et al. Blood. 2015;126(4):508-519.
Ungewikell et al. Nat Genet. 2015;47(9):1056-1060.
Choi J et al. Nat Genet. 2015;47(9):1011-1019.
Jawed SI et al. J Am Acad Dermatol. 2014;70(2):205.e1-16.
Kirsch IR et al. Sci Transl Med. 2015;7(308):308ra158.
Data on file, Helsinn Therapeutics US, Inc.
Osborne DW et al. AAPS PharmScitech. 2018;19(8):3512-3533.
Klucel^™ hydroxypropylcellulose. Ashland; Covington, KY. USA.
Sahu J et al. Clin Invest. 2014;4(8):745-761.

How VALCHLOR works: Mechanism of action and formulation

Mechlorethamine is an alkylating agent that inhibits rapidly proliferating cells1