To Determine the Effect of KP-001 on Rosuvastatin, Caffeine PK and the Effect of Fluvoxamine on KP-001 PK in Volunteers

NCT06821698 | Completed Phase 1 FDA Drug

• 1 other identifier: KP-001-106
• Study Type: interventional
• Target: 38
• Locations: 1 country
• Sites: 1

Brief Summary

Part 1 will evaluate the effects of KP-001 as an inhibitor of BCRP on the PK of rosuvastatin. In the Treatment Period 1, a single dose of rosuvastatin will be administered. In the Treatment Period 2, KP-001 will be administered once daily for 7 days and a single dose of rosuvastatin will be administered. Blood PK assessments of rosuvastatin will be performed until 48 hours postdose in each Treatment Period. Part 2 will evaluate the effects of KP-001 as an inducer and inhibitor of CYP1A2 on the PK of caffeine. A single dose of caffeine will be administered in the Treatment Period 1. KP-001 will be administered once daily for 10 days and a single dose of caffeine will be administered in the Treatment Period 2. Blood PK assessments of caffeine will be performed until 24 hours postdose in each Treatment Period. Part 3 will evaluate the effects of fluvoxamine as an inhibitor of CYP1A2 on the PK of KP-001. A single dose of KP-001 will be administered in the Treatment Period 1. Fluvoxamine will be administered as a single dose on the first day and then twice daily for 5 days and a single dose of KP-001 will be administered in the Treatment Period 2. Blood PK assessments of KP-001 will be performed until 48 hours postdose in each Treatment Period.

Conditions

Healty Volunteers

Outcome Measures

Primary Outcomes (6)

• PK parameters of rosuvastatin in plasma: AUCinf

  48hour

• PK parameters of rosuvastatin in plasma: Cmax

  48hour

• PK parameters of caffeine in plasma: AUCinf

  24hour

• PK parameters of caffeine in plasma: Cmax

  24hour

• PK parameters of KP-001 in plasma: AUCinf

  48hour

• PK parameters of KP-001 in plasma: Cmax

  48hour

Secondary Outcomes (14)

• PK parameters of rosuvastatin in plasma: AUClast

  48hour

• PK parameters of rosuvastatin in plasma: Tmax

  48hour

• PK parameters of rosuvastatin in plasma: t1/2

  48hour

• PK parameters of rosuvastatin in plasma: CLtot/F

  48hour

• PK parameters of rosuvastatin in plasma: Vz/F

  48hour

Study Arms (3)

KP-001/Rosuvastatin calcium

EXPERIMENTAL

Drug: KP-001; Drug: Rosuvastatin calcium10mg

KP-001/Caffeine citrate

EXPERIMENTAL

Drug: KP-001; Drug: Caffeine citrate

KP-001/Fluvoxamine

EXPERIMENTAL

Drug: KP-001; Drug: Fluvoxamine

Interventions

KP-001 DRUG

KP-001 100 mg dry syrup

KP-001/Caffeine citrate; KP-001/Fluvoxamine; KP-001/Rosuvastatin calcium

Rosuvastatin calcium10mg DRUG

A oral dose of 10 mg tablet

KP-001/Rosuvastatin calcium

Caffeine citrate DRUG

100 mg oral solution

KP-001/Caffeine citrate

Fluvoxamine DRUG

50 mg tablet

KP-001/Fluvoxamine

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• A participant who voluntarily agrees to participate in this study and signs an IRB-approved informed consent prior to performing any of the Screening Visit procedures.
• A male or female participant who is between 18 to 55 years of age, inclusive, at the Screening Visit.
• (Part 1 only) A participant who is non-Asian.
• A female participant who is non-childbearing potential defined in Section 10.4 and not pregnant or breastfeeding.
• A male participant who is sexually active with female partner(s) of childbearing potential must agree to use both a condom and spermicide from the first dose until 91 days after the last dose of KP-001.
• A male participant who agrees not to donate sperm from the first dose until 91 days after the last dose of KP-001.
• A continuous nonsmoker who has not used nicotine-containing products for at least 3 months prior to Day -1 of Treatment Period 1 and throughout the study, based on participant self-reporting and the result of cotinine test at screening and/or Day -1 of each Treatment Period.
• A participant who is medically healthy with no clinically significant abnormal screening results (eg, medical history, physical examination, laboratory profiles, vital signs, or ECGs), in the opinion of the Investigator or designee. If screening and/or admission results are abnormal, they may be repeated once at screening and/or once at admission to confirm the participant's eligibility.
• A participant who has body weight ≥ 50.0 kg and body mass index within the range 18.0 to 30.0 kg/m2, inclusive, at the Screening Visit.

You may not qualify if:

• A participant who is legally, mentally or physically incapacitated or, in the opinion of the Investigator, has significant mental or emotional problems, including psychiatric illness (eg, depression and/or anxiety) at the time of the Screening Visit, or that could reasonably be expected to develop during the conduct of the study.
• A participant with significant history or clinical manifestation of any metabolic, allergic, dermatologic, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, or psychiatric disorder as determined by the Investigator or designee.
• A participant with a history of any illness that, in the opinion of the Investigator or designee, might confound the results of the study or poses an additional risk to the participant by their participation in the study.
• (For Part 3 only) A participant who meets any of the following criteria based on the C-SSRS assessment at screening:
• Presence of suicidal ideation within the 6 months prior to screening (an answer of "yes" on Questions 1 or 2 of the C-SSRS Baseline/Screening version)
• Any lifetime history of suicidal ideation (an answer of "yes" on Questions 4 or 5 of the C-SSRS Baseline/Screening version).
• Any lifetime history of suicidal behavior as detected by the C-SSRS Baseline/Screening version.
• A participant who used any prescription or non-prescription medications (including vitamins, recreational drugs, and dietary or herbal supplements) within 14 days or 5 half-lives (whichever is longer) prior to Day -1 of Treatment Period 1 and until completion of the Follow-up Call unless, in the opinion of the Investigator, may be treatment for an AE or will not interfere with the interpretation of safety or the PK assessments.
• A participant who underwent blood donation or transfusion within 56 days prior to Day -1 of Treatment Period 1 and throughout the study.
• A participant with a history or presence of hypersensitivity or idiosyncratic reaction to any components of the KP-001 formulation or any components of formulation used as study intervention during the study.
• A participant with a history of drug or alcohol abuse (regular alcohol consumption exceeding 14 drinks/week \[1 drink=5 ounces of wine, 12 ounces of beer, or 1.5 ounces of hard liquor\]) within one year before the Screening Visit.
• A participant who has enrolled in any clinical study of KP-001.
• A participant with a complication of drug allergies or a history of drug allergies.
• A participant who used any investigational drug in the last 30 days or 5 half-lives (if known), whichever is longer, prior to Day -1 of Treatment Period 1.
• A participant who had any major illness within 30 days before the Screening Visit.

Sponsors & Collaborators

• Kaken Pharmaceutical: lead

Study Sites (1)

Parexel International Early Phase Clinical Unit

Glendale, California, 91206, United States

Location

MeSH Terms

Interventions

caffeine citrate; Fluvoxamine

Intervention Hierarchy (Ancestors)

Oximes; Hydroxylamines; Amines; Organic Chemicals

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 6, 2025
• First Posted: February 12, 2025
• Study Start: February 13, 2025
• Primary Completion: May 20, 2025
• Study Completion: May 20, 2025
• Last Updated: September 12, 2025

Record last verified: 2025-09

Locations

US (1)