Study of AC0058TA in Healthy Male and Female Subjects

NCT02847325 | Completed Phase 1

• 1 other identifier: AC00582015-101
• Study Type: interventional
• Target: 56
• Locations: 1 country
• Sites: 1

Brief Summary

AC0058TA is a small molecule compound that potently, selectively and irreversibly inhibits Bruton's tyrosine kinase (BTK) phosphorylation and downstream signals, resulting in inhibition of inflammatory cytokine production in monocytes and inhibition of lymphocyte activation (predominantly B-cell activation) in the preclinical studies. The nonclinical program has demonstrated that AC0058TA has the potential to interfere with signaling functions mediated by tyrosine kinases and may be useful for controlling excessive or aberrant T- and B-cell activation in autoimmune diseases. As an investigational targeted therapy for RA and SLE, AC0058TA is expected to address the unmet need of this patient population, for whom there are currently no effected therapies and there is a great unmet medical need, AC0058TA may inhibit the key pathway which involves the disease process.

Conditions

Healthy Volunteers

Outcome Measures

Primary Outcomes (1)

• Safety and tolerability of single and multiple oral doses of AC0058TA determined by adverse events

  Frequency and severity of AEs and serious AEs

  within 6 days after single dose in part 1, within 14 days after last dose in part 2.

Secondary Outcomes (4)

• Plasma concentrations of single dose or multiple doses of AC0058TA

  within 6 days after single dose in part 1, within 14 days after last dose in part 2.

• Time to maximum observed concentration (Tmax)

  within 6 days after single dose in part 1, within 14 days after last dose in part 2.

• Area under the concentration-time curve (AUC)

  within 6 days after single dose in part 1, within 14 days after last dose in part 2.

• The effect of food on AUC of the single-oral-dose AC0058TA

  within 6 days after single dose in part 1

Study Arms (2)

AC0058TA

EXPERIMENTAL

Drug: 50 mg AC0058TA Drug: 100 mg AC0058TA Drug: 200 mg AC0058TA Drug: 400 mg AC0058TA

Drug: AC0058TA

Placebo capsules

PLACEBO COMPARATOR

Drug: Placebo capsules

Drug: Placebo capsules

Interventions

AC0058TA DRUG

50 mg AC0058TA 100 mg AC0058TA 200 mg AC0058TA 400 mg AC0058TA

Also known as: AC0058

AC0058TA

Placebo capsules DRUG

Placebo capsules

Also known as: Placebo

Placebo capsules

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Male or female, of any ethnic origin, age ≥18 and ≤65 years of age;
• BMI ≥18.5 and ≤32.0 kg/m2;
• Medical history without major pathology and determined to be in good health with no clinically significant findings as assessed by the Investigator;
• All clinical laboratory tests of blood and urine are within the normal range or show no clinically relevant deviations as judged by the Investigator;
• A female must be
• postmenopausal (ie, have spontaneous amenorrhea for ≥12 consecutive months with follicle stimulating hormone (FSH) ≥40 mIU/mL at Screening, and be of an appropriate age) or
• surgically sterile (ie, hysterectomy, bilateral salpingectomy, bilateral oophorectomy, tubal occlusion) for at least 90 days prior to Screening;
• Male subjects must agree to use at least 2 methods of contraception with a female partner of childbearing potential, with at least 1 method being a highly effective method of contraception (as defined in Section 5.5), to refrain from sperm donation, and to refrain from unprotected sexual intercourse with a female who is pregnant or breastfeeding during the study from the time of signing the informed consent or 10 days prior to Check-in (Day -1) until 90 days after the last administration of study medication or discontinuation;
• Able to comprehend and abide by the study restrictions, and willing to sign an Informed Consent Form (ICF)

You may not qualify if:

• Has a significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, respiratory, endocrine, immune suppressive/defective, or psychiatric disorder as determined by the Investigator;
• Has a history of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance, unless approved by the Investigator;
• Has a history of stomach or intestinal surgery or resection that would potentially alter absorption and/or excretion of orally administered drugs (a subject who has had an appendectomy or hernia repair may be enrolled in the study);
• Has a history of congenital nonhemolytic hyperbilirubinaemia (eg, Gilbert's syndrome);
• Has a history of alcoholism or drug addiction within 1 year prior to Check-in;
• Has a positive test for selected drugs of abuse at Screening (not including alcohol) or Check-in (including alcohol);
• Has a positive hepatitis panel and/or positive human immunodeficiency virus (HIV) antibody screens;
• Has a positive pregnancy test result at Screening or Check-in (females only);
• Has clinically significant findings as determined by the Investigator (eg, medical history, 12-lead ECG, vital signs, or clinical laboratory evaluations;
• Has participated in any other investigational drug trial in which receipt of an investigational drug (new chemical entity) occurred within 5 half-lives of the respective study drug or 30 days prior to Check-in, whichever is longer;
• Has used any medications/products, including St. John's Wort, known to alter drug absorption or elimination processes within 30 days prior to Check-in, unless deemed acceptable by the Investigator;
• Has donated blood within 30 days prior to Screening, plasma within 2 weeks prior to Screening, or platelets within 6 weeks prior to Screening;
• Has received blood products within 2 months prior to Check-in;
• Has poor peripheral venous access;
• Who, in the opinion of the Investigator, should not participate in this study.

Sponsors & Collaborators

• ACEA Therapeutics, Inc.: lead

Study Sites (1)

Covance Clinical Development Services

Dallas, Texas, 75247, United States

Location

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 21, 2016
• First Posted: July 28, 2016
• Study Start: May 1, 2016
• Primary Completion: April 1, 2017
• Study Completion: April 1, 2017
• Last Updated: February 28, 2019

Record last verified: 2018-01

Locations

US (1)