tibremciclib (BPI-16350) / Betta Pharma - LARVOL DELTA

A phase I dose-escalation and dose-expansion study of tibremciclib, a novel CDK4/6 inhibitor, monotherapy and in combination with fulvestrant in HR-positive/HER2-negative advanced breast cancer. (PubMed, ESMO Open) - P1, P3 | "Tibremciclib monotherapy or combined with fulvestrant was well tolerated with the RP2D set at 400 mg plus fulvestrant 500 mg. PK was consistent with dose proportionality. Both regimens showed preliminary antitumor activity in patients with HR-positive/HER2-negative ABC, supporting further evaluation in a phase III study (NCT05433480)."

Journal • Monotherapy • P1 data • Breast Cancer • Dyslipidemia • Hematological Disorders • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Hypertriglyceridemia • Liposarcoma • Oncology • Sarcoma • Solid Tumor • CDK4 • HER-2

A Phase I Study of BPI-16350 in Patients with Advanced Solid Tumor (clinicaltrials.gov) - P1 | N=54 | Active, not recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd. | Recruiting ➔ Active, not recruiting | Trial completion date: Dec 2024 ➔ Dec 2025 | Trial primary completion date: Dec 2024 ➔ Dec 2025

Enrollment closed • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

Tibremciclib (BPI-16350) plus fulvestrant versus placebo plus fulvestrant for patients with HR+/HER2- advanced breast cancer after progressing on endocrine therapy: Updated analysis of the phase III study. (SABCS 2024) - P3 | "Tibremciclib plus fulvestrant continued to demonstrate a statistically significant and clinically meaningful improvement in PFS for patients with HR+/HER2- ABC who had progressed on endocrine therapy. Safety prolife was aligned with the previous interim analysis, with no new safety findings identified."

Clinical • Metastases • P3 data • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2

A Single-center, Open-label, Fixed-sequence, Drug-Drug Interaction Study of BPI-16350 co-administered with Rifampin or Itraconazole in Healthy Volunteers (ChiCTR) - P1 | N=36 | Completed | Sponsor: Beijing Friendship Hospital ,Capital Medical University; Beijing Friendship Hospital ,Capital Medical University

New P1 trial

Tibremciclib (BPI-16350) plus fulvestrant in patients with HR+/HER2- advanced breast cancer after progressing on endocrine therapy: A randomized, multicenter, double-blind, phase III study (ESMO 2024) - P1, P3 | "The study demonstrated a significant PFS benefit for tibremciclib with fulvestrant vs placebo fulvestrant and had a good safety profile in pts with HR+/HER2- ABC after progression on ET."

Clinical • Metastases • P3 data • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Beida Pharmaceuticals (300558.SZ): BPI-16350 drug registration application accepted [Google translation] (Zhitong Finance) - "According to the Zhitong Finance APP, Beida Pharmaceutical...announced that the company has received the 'Acceptance Notice' issued by the National Medical Products Administration ('NMPA'), and the company's application for marketing authorization of BPI-16350 (Tibremciclib Tartrate Capsules). 'This product, combined with Fulvestrant, is suitable for the treatment of patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or late recurrent metastatic breast cancer that has progressed after previous endocrine therapy' has been accepted by NMPA."

New trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

A Study of BPI-16350 in Combination With Fulvestrant in Patients With HR+ and HER2- Locally Advanced, Recurrent or Metastatic Breast Cancer (clinicaltrials.gov) - P3 | N=274 | Active, not recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd. | Not yet recruiting ➔ Active, not recruiting

Enrollment closed • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2

BPI-16350, a novel promising CDK4/6 inhibitor for HR+/HER2- metastatic breast cancer (MBC): Results from a phase I study. (ASCO 2023) - P1, P3 | "This is an open-label, dose-escalation and -expansion phase I study to evaluate the safety, pharmacokinetics, and preliminary antitumor activity of BPI-16350 as monotherapy (Part A) and combined treatment with fulvestrant (FUL) in pts with HR+/HER2- MBC (Part B)...Pts in this part should have received no more than one line of chemotherapy for metastatic disease and no prior therapies with other CDK4/6 inhibitors, FUL or everolimus... To our knowledge, BPI-16350 plus FUL demonstrated numerically highest antitumor activity compared with the already approved CDK4/6 inhibitors and less Grade ≥ 3 diarrhea than abemaciclib. A phase III study (NCT05433480) comparing BPI-16350 plus FUL versus placebo plus FUL in pts with MBC is ongoing. Clinical trial information: NCT03791112."

Metastases • P1 data • Anemia • Breast Cancer • Hematological Disorders • HER2 Breast Cancer • Leukopenia • Liposarcoma • Neutropenia • Oncology • Sarcoma • Solid Tumor • CDK9 • HER-2

A Food-Effect Study of BPI-16350 in Healthy Subjects (clinicaltrials.gov) - P1 | N=24 | Completed | Sponsor: Betta Pharmaceuticals Co., Ltd. | Active, not recruiting ➔ Completed

Trial completion

A Study of BPI-16350 in Combination With Fulvestrant in Patients With HR+ and HER2- Locally Advanced, Recurrent or Metastatic Breast Cancer (clinicaltrials.gov) - P3 | N=267 | Not yet recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd.

Combination therapy • New P3 trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2

A Food-Effect Study of BPI-16350 in Healthy Subjects (clinicaltrials.gov) - P1 | N=24 | Active, not recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd. | Recruiting ➔ Active, not recruiting

Enrollment closed

A Phase I Study of BPI-16350 in Patients With Advanced Solid Tumor (clinicaltrials.gov) - P1 | N=54 | Recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd. | Unknown status ➔ Recruiting | Trial completion date: Dec 2021 ➔ Dec 2024 | Trial primary completion date: Jun 2021 ➔ Dec 2024

Enrollment open • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

A Food-Effect Study of BPI-16350 in Healthy Subjects (clinicaltrials.gov) - P1 | N=24 | Recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open

BPI-421286: A highly potent small molecule inhibitor targeting KRASG12C mutation (AACR 2022) - "Combining BPI-421286 with several targeted agents, including a SHP2 inhibitor BPI-442096 and a CDK4/6 inhibitor BPI-16350, demonstrated enhanced tumor growth inhibition compared to either agent alone. Taken together, BPI-421286 is a highly potent and selective KRASG12C inhibitor, with favorable ADME properties and wide therapeutic index in pre-clinical toxicology studies. BPI-421286 is currently in Phase 1 clinical study."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • KRAS

A Phase 1 Food-Effect Study of BPI-16350 in Healthy Subjects (clinicaltrials.gov) - P1 | N=24 | Not yet recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd.

New P1 trial