JAK1 inhibitor cream (ARQ-252)

Overview

Janus kinase 1 (JAK1) inhibitor cream (ARQ-252) is being investigated for the treatment of chronic hand eczema and vitiligo.

ARQ-252 is a selective, highly potent,* topical JAK1 inhibitor that demonstrates greater in vitro potency for JAK1 than JAK2.1

*In vitro data. Clinical efficacy claims cannot be made.

Chronic hand eczema

Topical JAK1 inhibitor cream (ARQ-252) in chronic hand eczema.

Clinical landscape

  • Chronic hand eczema is a form of eczema that is located on the hands and/or wrists. Symptoms may include itching, burning, crusting, and scaling2
  • Chronic hand eczema may negatively affect quality of life, and incurs a substantial economic burden (eg, reduced work productivity)3,4
  • A considerable unmet need exists for new therapies for hand eczema since few therapies are approved4

Proposed MOA

  • Inhibition of JAK has been shown to reduce pruritus in vitro5
  • ARQ-252 is a selective, highly potent,* topical, small-molecule JAK1 inhibitor that is being investigated for the treatment of chronic hand eczema1

*In vitro data. Clinical efficacy claims cannot be made.

MOA = mechanism of action

Clinical programs

Phase 1/2

A phase 1/2b study of ARQ-252 in chronic hand eczema has been completed.

ClinicalTrials.gov identifier: NCT04378569

Summary of results

  • The primary endpoint was not met, with none of the ARQ-252 cohorts achieving statistical significance vs vehicle
  • Reformulation is underway to improve local drug delivery to the skin
View Study Details
Vitiligo

Topical JAK1 inhibitor cream (ARQ-252) in vitiligo.

Clinical landscape

  • Vitiligo is an autoimmune condition characterized by the appearance of white macules on the skin as a result of the selective loss of melanocytes6
  • There are limited approved therapies to treat vitiligo
  • Physician-recommended therapies include narrow-band ultraviolet B, tacrolimus, and topical steroids7

Proposed MOA

  • Repigmentation of the skin has been demonstrated in some patients with vitiligo following inhibition of the JAK signal transducer and activator of transcription (STAT) pathway8
  • ARQ-252 is a selective, highly potent,* topical, small-molecule JAK1 inhibitor that is being investigated for the treatment of vitiligo1

*In vitro data. Clinical efficacy claims cannot be made.

MOA = mechanism of action

Clinical programs

Phase 2

A phase 2a trial of topical JAK inhibitor cream in nonsegmental facial vitiligo has been terminated.

ClinicalTrials.gov identifier: NCT04811131

Summary of results

  • Decision to terminate was based on analyses of the formulation used in both this vitiligo study and the recently completed phase 2b chronic hand eczema study
  • Analyses of the chronic hand eczema study pointed toward inadequate local drug delivery to the skin as a key driver of the lack of efficacy
  • The vitiligo study was not terminated for safety or tolerability reasons
  • Reformulation is underway to improve local drug delivery to the skin
View Study Details
References

1. Data on File. Arcutis Biotherapeutics, Inc. 2. Agner and Elsner. JEADV. 2020;34(Suppl. 1):4-12. 3. Bingefors et al. Acta Derm Venereol. 2011;91:452-458. 4. Dibenedetti et al. J Clin Aesthet Dermatol. 2015;8:19-27. 5. Howell et al. Front Immunol. 2019;10:2342. 6. Bergqvist and Ezzedine. Dermatology. 2020;236:571-592. 7. Ezzedine et al. Lancet. 2015;386:74-84. 8. Liu et al. J Am Acad Dermatol. 2017;77:675-682.

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This website is intended for US healthcare professionals only. There may be information included that pertains to an investigational therapy or formulation that has not yet been approved for use in your country. The safety and efficacy of investigational therapies and/or formulations and/or uses have not been established. There is no guarantee that the agents will receive health authority approval or become commercially available in any country for the uses being investigated. This information is as of 7/2024 to the best of the Company’s knowledge and Arcutis assumes no obligation to update this information.

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