Efficacy and Safety of Tenalisib (RP6530), a PI3K δ/γ and SIK3 Inhibitor, in Patients With Locally Advanced or Metastatic Breast Cancer

A Phase II, Multi-center, Randomized, Open-label, Two-arm Study to Assess the Efficacy and Safety of Tenalisib (RP6530), a PI3K δ/γ and SIK3 Inhibitor, in Patients With Locally Advanced or Metastatic Breast Cancer

Phase II, randomized, open-label study, designed to evaluate the preliminary efficacy and safety of tenalisib at two dose levels in 40 patients with locally advanced or metastatic breast cancer.

Study Overview

• Status: Completed
• Conditions: Metastatic Breast Cancer; Locally Advanced Breast Cancer
• Intervention / Treatment: Drug: Tenalisib; Drug: Tenalisib

• Study Type: Interventional
• Enrollment (Actual): 40
• Phase: Phase 2

Contacts and Locations

Study Locations

• Georgia
  • Batumi, Georgia
    • High Technology Hospital Medcenter
  • Tbilisi, Georgia, 0186
    • LLC Caucasus Medical Center
  • Tbilisi, Georgia
    • Simon Khechinashvili University Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years and older (Adult, Older Adult)
• Accepts Healthy Volunteers: No

Description

Inclusion Criteria:

1. Patients must be ≥18 years of age, at the time of signing informed consent.
2. Female patients who have histologically and/or cytologically confirmed locally advanced or metastatic breast cancer that has progressed following at least one line of therapy.
3. Patients with at least one measurable lesion per RECIST version 1.1 at baseline that can be accurately assessed by CT scan or MRI and is suitable for repeated assessment at follow up-visits.
4. ECOG performance status 0 to 2.
5. Life expectancy of at least 3 months.
6. Adequate bone marrow, liver, and renal functions
7. Female patients of childbearing potential should be willing to use a medically acceptable method of contraception

Exclusion Criteria:

1. Patients with HER-2 positive breast cancer.
2. Patients receiving anticancer therapy within 4 weeks or 5 half-lives of the drug prior to C1D1, whichever is shorter.
3. Patient who has not recovered from acute toxicities (defined as NCI-CTCAE grade > 1) of previous therapy except treatment-related alopecia.
4. Patients who have had disease progression within 8 weeks of platinum chemotherapy.
5. Prior exposure to investigational or marketed PI3K inhibitors given for the treatment of breast cancer.
6. Major surgery within 4 weeks of starting study treatment OR any patient who has not recovered from the effects of major surgery.
7. Patient with symptomatic uncontrolled brain metastasis.
8. HIV-positive patients who are on antiretroviral therapy OR active hepatitis C OR active hepatitis B virus infections.
9. Ongoing immunosuppressive therapy including systemic corticosteroids except as allowed per concomitant medication.
10. Known history of severe liver injury as judged by the investigator.
11. History of severe cutaneous reactions in the past.
12. Active gastrointestinal tract disease with malabsorption syndrome or uncontrolled inflammatory gastrointestinal disease such as Crohn's disease or ulcerative colitis.
13. Pregnancy or lactation.
14. Patient with other active malignancies at the time of screening.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Tenalisib 800 mg BID	Drug: Tenalisib; Tenalisib will be administered 800mg BID, orally; Drug: Tenalisib; Tenalisib will be administered 1200mg BID, orally
Experimental: Tenalisib 1200 mg BID	Drug: Tenalisib; Tenalisib will be administered 800mg BID, orally; Drug: Tenalisib; Tenalisib will be administered 1200mg BID, orally

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Percentage of patients without disease progression	6 months

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Overall Response Rate (ORR)	It is defined as sum of CR and PR rates	2 years
Clinical Benefit Rate (CBR)	It is defined as sum of CR, PR and SD rates	2 years
Progression Free Survival (PFS).	PFS is measured from the time of first dose of study drug to radiographic documentation of disease progression or death due to any cause.	2 years
Treatment emergent adverse events (TEAEs)		2 years

Collaborators and Investigators

• Sponsor: Rhizen Pharmaceuticals SA

Study record dates

Study Major Dates

• Study Start (Actual): October 13, 2021
• Primary Completion (Actual): March 31, 2023
• Study Completion (Actual): March 31, 2023

Study Registration Dates

• First Submitted: August 19, 2021
• First Submitted That Met QC Criteria: August 19, 2021
• First Posted (Actual): August 26, 2021

Study Record Updates

• Last Update Posted (Actual): May 17, 2023
• Last Update Submitted That Met QC Criteria: May 16, 2023
• Last Verified: May 1, 2023

More Information

Terms related to this study

• Keywords: Tenalisib; RP6530
• Additional Relevant MeSH Terms: Skin Diseases; Neoplasms; Neoplasms by Site; Breast Diseases; Breast Neoplasms; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Phosphoinositide-3 Kinase Inhibitors; Tenalisib
• Other Study ID Numbers: RP6530-2101

Drug and device information, study documents

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