JAK1 Inhibitor ARQ-252 Cream

ARQ-252 is a selective, highly potent, topical Janus kinase 1 (JAK1) inhibitor being investigated as a cream for the treatment of hand eczema and vitiligo.

  • ARQ-252 demonstrates greater potency in vitro for JAK1 than JAK2,1 which may avoid the hematologic adverse effects typically associated with inhibition of JAK22
  • Selective inhibition of JAKs in development has demonstrated treatment efficacy for inflammatory conditions such as rheumatoid arthritis, Crohn’s disease, psoriasis, and atopic dermatitis3

Topical JAK1 Inhibitor Cream (ARQ-252) in Hand Eczema

Landscape

  • Chronic hand eczema is a common condition that occurs in different forms,4 negatively affects quality of life, and incurs a substantial economic burden (eg, reduced work productivity)5,6
  • A considerable unmet need exists for new therapies for hand eczema since few therapies are approved and most patients and physicians are not satisfied with treatment options6

Mechanism

  • Inhibition of JAK has been shown to reduce pruritus in vitro7
  • ARQ-252 is a selective, highly potent, topical, small-molecule JAK1 inhibitor that is being investigated for the treatment of hand eczema
Hand with eczema.

Development

Phase 1/2b study has been completed (NCT04378569)

Infographic showing eligibility, 2 week dosing and 1 week follow up, 8 week dosing, and endpoints of phase 1/2b ongoing study.

aIGA success was defined as scores of 0 or 1 (clear or almost clear) with at least a 2-grade improvement from baseline.
BID, twice daily; BSA, body surface area; IGA, Investigator's Global Assessment; QD, once daily; WI-NRS, Worst Itch Numeric Rating Scale.

Topical JAK1 Inhibitor Cream (ARQ-252) in Vitiligo

Landscape

  • There are no FDA-approved therapies to treat vitiligo
  • Physician-recommended therapies include narrow-band ultraviolet B, tacrolimus, and topical steroids8
  • Because of limited treatment options, a critical need exists for safe effective drug therapies for vitiligo8

Mechanism

  • Inhibition of the JAK–signal transducer and activator of transcription (STAT) pathway induces successful repigmentation in vitiligo9
  • ARQ-252 is a selective, highly potent, topical, small-molecule JAK1 inhibitor that is being investigated for the treatment of vitiligo
Dark haired woman with vitiligo on her face.

Development

Phase 2a trial of topical JAK inhibitor cream in nonsegmental facial vitiligo is ongoing (NCT04811131)

Infographic showing eligibility, 24 week dosing and endpoints of phase 2a study.

BID, twice daily; BSA, body surface area; F-VASI, Facial Vitiligo Area Scoring Index; FsIGA, Facial Static Investigator’s Assessment; PaGIC-V, Patient Global Impression of Change-Vitiligo; VitiQoL, Vitiligo-Specific Quality-of-Life Instrument; VNS, Vitiligo Noticeability Scale.

References

1. Data on file, Arcutis Biotherapeutics. 2. Biggioggero et al. Drugs Context. 2019;8:212595. 3. Damsky and King. J Am Acad Dermatol. 2017;76:736-744. 4. Diepgen et al. Br J Dermatol. 2009;160:353-358. 5. Bingefors et al. Acta Derm Venereol. 2011;91:452-458. 6. Dibenedetti et al. J Clin Aesthet Dermatol. 2015;8:19-27. 7. Howell et al. Front Immunol. 2019;10:2342. 8. Ezzedine et al. Lancet. 2015;386:74-84. 9. Liu et al. J Am Acad Dermatol. 2017;77:675-682.

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