NCT03918980

Single Dose and Multiple Dose Study to Assess Safety and Tolerability of LOU064

Completed Phase 1 Last updated 12 October 2021

What this trial tests

Phase 1 trial testing LOU064 in Healthy Volunteers, Atopic Diathesis and Atopic Dermatitis in 185 participants. Completed in 27 January 2020.

Timeline

18 August 2016

Primary endpoint
27 January 2020

27 January 2020

Quick facts

Lead sponsor	Novartis Pharmaceuticals
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	parallel
Masking	triple
Primary purpose	treatment
Enrollment	185
Start date	18 August 2016
Primary completion	27 January 2020
Estimated completion	27 January 2020
Sites	2 locations across Netherlands, Germany

Drugs / interventions tested

• LOU064 — full drug profile →
• Placebo

Conditions studied

• Healthy Volunteers, Atopic Diathesis and Atopic Dermatitis — all drugs for Healthy Volunteers, Atopic Diathesis and Atopic Dermatitis →

Sponsor

Novartis Pharmaceuticals — full company profile →

Who can join

Adults 18 to 65, any sex, with Healthy Volunteers, Atopic Diathesis and Atopic Dermatitis. Patients with the condition only — healthy volunteers not accepted.

Sponsor's own description

This is a 6-part first-in-human study in up to approximately 184 participants. Parts 1 to 5 is in health volunteers and part 6 is in subjects with atopic dermatitis.

The purpose of this first-in-human study is to assess the safety and tolerability and pharmacokinetics (PK) of single and multiple doses of LOU064 both as once and twice daily oral administration in healthy volunteers and those with atopic diathesis or atopic dermatitis. This study will also explore the effect of food intake and different drug substance particle sizes on the in vivo disposition of LOU064 in healthy volunteers to guide dosing and formulation development for future clinical trials.

The study is registered on CT.Gov with the initiation of part 6 in patients (FPFV in April 2019).

Publications & conference data

6 peer-reviewed publications reference this trial (live from Europe PMC):

1. Bruton's tyrosine kinase inhibition-An emerging therapeutic strategy in immune-mediated dermatological conditions.
   Mendes-Bastos P, Brasileiro A, Kolkhir P, Frischbutter S, et al · · 2022 · cited 67× · PMID 35175630 · DOI 10.1111/all.15261
2. Remibrutinib (LOU064): A selective potent oral BTK inhibitor with promising clinical safety and pharmacodynamics in a randomized phase I trial.
   Kaul M, End P, Cabanski M, Schuhler C, et al · · 2021 · cited 59× · PMID 33834628 · DOI 10.1111/cts.13005
3. Bruton's Kinase Inhibitors for the Treatment of Immunological Diseases: Current Status and Perspectives.
   Robak E, Robak T. · · 2022 · cited 45× · PMID 35628931 · DOI 10.3390/jcm11102807
4. Recent Advances in BTK Inhibitors for the Treatment of Inflammatory and Autoimmune Diseases.
   Zhang D, Gong H, Meng F. · · 2021 · cited 45× · PMID 34443496 · DOI 10.3390/molecules26164907
5. Bruton's Tyrosine Kinase Inhibitors in Multiple Sclerosis: Pioneering the Path Towards Treatment of Progression?
   Geladaris A, Torke S, Weber MS. · · 2022 · cited 22× · PMID 36178589 · DOI 10.1007/s40263-022-00951-z
6. Novel Bruton's Tyrosine Kinase inhibitor remibrutinib: Drug-drug interaction potential as a victim of CYP3A4 inhibitors based on clinical data and PBPK modeling.
   Huth F, Schiller H, Jin Y, Poller B, et al · · 2022 · cited 9× · PMID 34432364 · DOI 10.1111/cts.13126