A Study Investigating the Safety of RO7795081 and the Effect of RO7795081 on How the Body Processes Pitavastatin and Rosuvastatin in Otherwise Healthy Overweight or Obese Adult Participants

A Phase I, Randomized, Investigator/Participant-Blind, Placebo-Controlled, Fixed-Sequence Study to Investigate the Safety, Tolerability, and Pharmacokinetics of Multiple Doses of Orally Administered RO7795081 and the Effect of Steady-State Dose of Orally Administered RO7795081 on the Pharmacokinetics of Pitavastatin and Rosuvastatin in Otherwise Healthy Overweight or Obese Adult Participants

This is a randomized, investigator-and-participant-blind, placebo-controlled, fixed sequence, cross-over, Phase 1 study to investigate the safety, tolerability, and pharmacokinetics of multiple doses of orally administered RO7795081 and the effect of a steady-state dose of orally administered RO7795081 on the pharmacokinetics of pitavastatin and rosuvastatin in otherwise healthy, overweight or obese adult participants.

Study Overview

• Status: Recruiting
• Conditions: Obesity; Overweight
• Intervention / Treatment: Drug: RO7795081; Drug: Rosuvastatin; Drug: Pitavastatin; Drug: Placebo

• Study Type: Interventional
• Enrollment (Estimated): 40
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Reference Study ID Number: BP45800 https://forpatients.roche.com/; Phone Number: 888-662-6728 (U.S. Only); Email: global-roche-genentech-trials@gene.com
• Study Contact Backup: Name: Fastest response: use the inquiry form. No email attachments. https://www.gene.com/contact-us/submit-medical-inquiry

Study Locations

• Netherlands
  • Groningen, Netherlands, 9728 NZ
    • Recruiting
    • ICON Plc (LPRA) - Netherlands

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Healthy participants with no clinically relevant findings on physical examination at screening and at baseline (including detailed medical and surgical history, vital signs, 12-lead ECG, hematology, blood chemistry, and urinalysis); with no suspicion of cognitive impairment or dementia as judged by the Investigator; who are not under judicial supervision, guardianship, or curatorship.
• Body Mass Index (BMI) ≥27.0 kg/m^2 at screening and on Day -1 of Period 1
• Stable body weight (defined as <5% gain or loss) in the 2 months prior to screening as per verbal report by the participant and for the period between screening and Day -1 of Period 1 as per measured weight
• Agreement to adhere to the contraception requirements

Exclusion Criteria:

• Pregnant, breastfeeding, or intending to become pregnant during the study
• Any condition or disease detected during the medical interview or physical examination that would render the participant unsuitable for the study, place the participant at undue risk, or interfere with the ability of the participant to complete the study in the opinion of the Investigator
• History or presence of any clinically significant cardiovascular, broncho-pulmonary, hepatic, renal, gastrointestinal, endocrinological, hematological, neurological, psychiatric, or metabolic disorders, allergic diseases, hypofertility, cancer, or cirrhosis
• History or evidence of any medical condition capable of significantly altering the absorption, metabolism, or elimination of drugs
• History of convulsions (other than benign febrile convulsions of childhood) including epilepsy, or personal history of significant cerebral trauma or CNS infections (e.g., meningitis)
• History of acute or chronic metabolic acidosis, including diabetic ketoacidosis with or without coma

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: Double

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Arm 1: ROS Alone, Then PIT Alone, Then RO7795081 Alone, Then RO7795081 + ROS, Then RO7795081 + PIT; Period 1: Rosuvastatin (ROS) alone; Period 2: Pitavastatin (PIT) alone; Period 3: RO7795081 alone; Period 4: RO7795081 in combination with ROS; Period 5: RO7795081 in combination with PIT	Drug: RO7795081; RO7795081 will be administered orally during Periods 3, 4, and 5, according to the protocol.; Other Names: CT-996; RG6652; Drug: Rosuvastatin; A single 10 mg dose of rosuvastatin (ROS) will be taken on Day 1 of Period 1 and on Day 1 of Period 4.; Other Names: Crestor®; Drug: Pitavastatin; A single 1 mg dose of pitavastatin (PIT) will be taken on Day 1 of Period 2 and on Day 1 of Period 5.; Other Names: Livalo®; Livazo®; Zypitamag®
Placebo Comparator: Arm 2: ROS Alone, Then PIT Alone, Then Placebo Alone, Then Placebo + ROS, Then Placebo + PIT; Period 1: Rosuvastatin (ROS) alone; Period 2: Pitavastatin (PIT) alone; Period 3: Placebo alone; Period 4: Placebo in combination with ROS; Period 5: Placebo in combination with PIT	Drug: Rosuvastatin; A single 10 mg dose of rosuvastatin (ROS) will be taken on Day 1 of Period 1 and on Day 1 of Period 4.; Other Names: Crestor®; Drug: Pitavastatin; A single 1 mg dose of pitavastatin (PIT) will be taken on Day 1 of Period 2 and on Day 1 of Period 5.; Other Names: Livalo®; Livazo®; Zypitamag®; Drug: Placebo; Placebo will be administered orally during Periods 3, 4, and 5, according to the protocol.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Incidence and Severity of Adverse Events	From the first dose of study treatment until the final visit (up to 111 days)
Incidence of Abnormal Clinical Laboratory Test Results	From the first dose of study treatment until the final visit (up to 111 days)
Incidence of Abnormal Vital Sign Assessments	From the first dose of study treatment until the final visit (up to 111 days)
Incidence of Abnormal Electrocardiogram Parameters	From the first dose of study treatment until the final visit (up to 111 days)
Maximum Plasma Concentration Observed (Cmax) of Rosuvastatin, Administered Alone and in Combination with RO7795081	Periods 1 and 4: predose and postdose at prespecified times on Days 1 to 5
Time to Maximum Plasma Concentration (Tmax) of Rosuvastatin, Administered Alone and in Combination with RO7795081	Periods 1 and 4: predose and postdose at prespecified times on Days 1 to 5
Area Under the Plasma Concentration-Time Curve (AUC) from Time 0 to the Last Measurable Concentration (AUClast) of Rosuvastatin, Administered Alone and in Combination with RO7795081	Periods 1 and 4: predose and postdose at prespecified times on Days 1 to 5
AUC from Time 0 to Infinity (AUCinf) of Rosuvastatin, Administered Alone and in Combination with RO7795081	Periods 1 and 4: predose and postdose at prespecified times on Days 1 to 5
Cmax of Pitavastatin, Administered Alone and in Combination with RO7795081	Periods 2 and 5: predose and postdose at prespecified times on Days 1 to 4
Tmax of Pitavastatin, Administered Alone and in Combination with RO7795081	Periods 2 and 5: predose and postdose at prespecified times on Days 1 to 4
AUClast of Pitavastatin, Administered Alone and in Combination with RO7795081	Periods 2 and 5: predose and postdose at prespecified times on Days 1 to 4
AUCinf of Pitavastatin, Administered Alone and in Combination with RO7795081	Periods 2 and 5: predose and postdose at prespecified times on Days 1 to 4

Secondary Outcome Measures

Outcome Measure	Time Frame
Plasma Concentration of RO7795081 Over Time, Administered Alone and in Combination with Rosuvastatin and Pitavastatin	Period 3: predose and postdose at prespecified times from Days 2 to 49; Period 4: predose and postdose at prespecified times on Days 1 to 4; Periods 4: predose and postdose at prespecified times on Days 1 to 9
Cmax of RO7795081, Administered Alone and in Combination with Rosuvastatin and Pitavastatin	Period 3: predose and postdose at prespecified times from Days 2 to 49; Period 4: predose and postdose at prespecified times on Days 1 to 4; Periods 4: predose and postdose at prespecified times on Days 1 to 9
Tmax of RO7795081, Administered Alone and in Combination with Rosuvastatin and Pitavastatin	Period 3: predose and postdose at prespecified times from Days 2 to 49; Period 4: predose and postdose at prespecified times on Days 1 to 4; Periods 4: predose and postdose at prespecified times on Days 1 to 9
AUClast of RO7795081, Administered Alone and in Combination with Rosuvastatin and Pitavastatin	Period 3: predose and postdose at prespecified times from Days 2 to 49; Period 4: predose and postdose at prespecified times on Days 1 to 4; Periods 4: predose and postdose at prespecified times on Days 1 to 9
AUCinf of RO7795081, Administered Alone and in Combination with Rosuvastatin and Pitavastatin	Period 3: predose and postdose at prespecified times from Days 2 to 49; Period 4: predose and postdose at prespecified times on Days 1 to 4; Periods 4: predose and postdose at prespecified times on Days 1 to 9

Collaborators and Investigators

• Sponsor: Hoffmann-La Roche
• Investigators: Study Director: Clinical Trials, Hoffmann-La Roche

Publications and helpful links

Helpful Links

• Please use this form to submit your questions for a faster response: https://www.gene.com/contact-us/submit-medical-inquiry. Do not include or attach any medical records when emailing or completing the form. A nurse will respond within 24 business hours.

Study record dates

Study Major Dates

• Study Start (Actual): June 4, 2025
• Primary Completion (Estimated): December 4, 2026
• Study Completion (Estimated): December 4, 2026

Study Registration Dates

• First Submitted: May 13, 2025
• First Submitted That Met QC Criteria: May 13, 2025
• First Posted (Actual): May 21, 2025

Study Record Updates

• Last Update Posted (Actual): June 4, 2026
• Last Update Submitted That Met QC Criteria: June 3, 2026
• Last Verified: June 1, 2026

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Nutrition Disorders; Overnutrition; Body Weight; Pathological Conditions, Signs and Symptoms; Nutritional and Metabolic Diseases; Signs and Symptoms; Overweight; Obesity; Sulfur Compounds; Organic Chemicals; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Hydrocarbons; Amides; Pyrimidines; Hydrocarbons, Halogenated; Sulfonamides; Sulfones; Fluorobenzenes; Hydrocarbons, Fluorinated; Rosuvastatin Calcium; pitavastatin
• Other Study ID Numbers: BP45800; 2024-519277-18-00 (Ctis)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No