^
    6d
    A Study of Rocbrutinib in Participants with Relapse or Refractory Mantle Cell Lymphoma (clinicaltrials.gov)
    P2, N=62, Active, not recruiting, Guangzhou Lupeng Pharmaceutical Company LTD. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    rocbrutinib (LP-168)
    2ms
    A Study of Rocbrutinib in Participants with Relapse or Refractory Mantle Cell Lymphoma (clinicaltrials.gov)
    P2, N=62, Recruiting, Guangzhou Lupeng Pharmaceutical Company LTD. | Trial primary completion date: Feb 2024 --> Dec 2024
    Trial primary completion date
    |
    rocbrutinib (LP-168)
    2ms
    A Study of LP-168 in Participants with Relapse or Refractory B-Cell Lymphoma (clinicaltrials.gov)
    P1, N=200, Recruiting, Guangzhou Lupeng Pharmaceutical Company LTD. | Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial completion date • Trial primary completion date
    |
    rocbrutinib (LP-168)
    8ms
    LP-168-CN301: Phase Ib Study of Rocbrutinib in Combination With R-CHOP in Patients With Newly Diagnosed B-cell Non-Hodgkin Lymphoma (clinicaltrials.gov)
    P1, N=112, Recruiting, Guangzhou Lupeng Pharmaceutical Company LTD. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy
    |
    Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • prednisone • rocbrutinib (LP-168)
    9ms
    The Mass Balance Study of LP-168 in Healthy Subjects (clinicaltrials.gov)
    P1, N=6, Completed, Guangzhou Lupeng Pharmaceutical Company LTD. | Active, not recruiting --> Completed
    Trial completion
    |
    rocbrutinib (LP-168)
    10ms
    The Mass Balance Study of LP-168 in Healthy Subjects (clinicaltrials.gov)
    P1, N=6, Active, not recruiting, Guangzhou Lupeng Pharmaceutical Company LTD. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    rocbrutinib (LP-168)
    11ms
    Phase Ib Study of Rocbrutinib in Combination With R-CHOP in Patients With Newly Diagnosed B-cell Non-Hodgkin Lymphoma (clinicaltrials.gov)
    P1, N=112, Not yet recruiting, Guangzhou Lupeng Pharmaceutical Company LTD.
    New P1 trial
    |
    Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • prednisone • rocbrutinib (LP-168)
    12ms
    The Mass Balance Study of LP-168 in Healthy Subjects (clinicaltrials.gov)
    P1, N=8, Recruiting, Guangzhou Lupeng Pharmaceutical Company LTD. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    rocbrutinib (LP-168)
    1year
    Study of Oral Administration of LP-168 in Patients With Relapsed or Refractory B-cell Malignancies. (clinicaltrials.gov)
    P1, N=60, Recruiting, Newave Pharmaceutical Inc | Trial completion date: Jul 2023 --> Dec 2025 | Trial primary completion date: Jul 2023 --> Jul 2025
    Trial completion date • Trial primary completion date
    |
    rocbrutinib (LP-168)
    1year
    The Mass Balance Study of LP-168 in Healthy Subjects (clinicaltrials.gov)
    P1, N=8, Not yet recruiting, Guangzhou Lupeng Pharmaceutical Company LTD.
    New P1 trial
    |
    rocbrutinib (LP-168)
    1year
    Pre-Clinical Evaluation of a New-Generation Orally Bioavailable Dual Bcl-2/Bcl-Xl Inhibitor LP-118 in Mantle Cell Lymphoma (ASH 2023)
    For in vivo experiments, Granta519 and REC-1-derived xenograft models were established and treated with different regimens: for Granta519 model, mice were treated with vehicle, BR (bendamustine, 25mg/kg, iv, day 1 and rituximab, 10mg/kg, iv, day 1), LP-118 (75mg/kg, po, qd, 28 days) in combination with BR...In the matrix combination studies with REC-1 cells, combinations of LP-118 with SOC agents showed synergistic anticancer effects with all the tested drugs, including vincristine, bendamustine, cytarabine, docetaxel, doxorubicin, cisplatin, and bortezomib...Similarly, the combination of LP-118 with LP-168 (BTKi) also resulted in complete tumor regression in REC-1 xenograft models at day 40, while the combination of ABT-199 plus ibrutinib showed no significant tumor growth inhibition, suggesting that combination of LP-118 and LP-168, a new generation BTKi currently also in clinical trial, might be more effective against MCL than the combination of ABT-199 plus ibrutinib in clinic. Conclusion LP-118 showed encouraging anti-MCL activity as single agent and in combination with standard of care agents in vitro and in vivo, warranting further evaluation of these combinations in clinical trials.
    Preclinical • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1)
    |
    Venclexta (venetoclax) • cisplatin • Imbruvica (ibrutinib) • Rituxan (rituximab) • docetaxel • cytarabine • bortezomib • doxorubicin hydrochloride • vincristine • bendamustine • LP-118 • rocbrutinib (LP-168)
    1year
    Initial Results of a Phase 1 Dose Escalation Study of LP-168, a Novel Covalent and Non-Covalent Next-Generation Inhibitor of Bruton's Tyrosine Kinase (ASH 2023)
    Covalent BTKi (cBTKi) including ibrutinib, acalabrutinib, and zanubrutinib, share a common resistance mechanism, acquisition of a C481 mutation in BTK. LP-168 has been well tolerated in this study, with no DLTs identified at doses up to 300 mg daily. Preliminary efficacy was observed in high risk CLL pts, including those treated with one or more BTKi. Considering safety, efficacy, and PK/PD, dose expansion will occur at 200 mg and 300 mg daily following the FDA Project Optimus guidelines to determine the recommended phase 2 dose.
    P1 data
    |
    TP53 (Tumor protein P53) • PLCG2 (Phospholipase C Gamma 2)
    |
    BTK C481S • BTK mutation • BTK C481
    |
    Imbruvica (ibrutinib) • Brukinsa (zanubrutinib) • Calquence (acalabrutinib) • rocbrutinib (LP-168)
    over1year
    A Food Effect Study of LP-168 Tablets in Healthy Subjects (clinicaltrials.gov)
    P1, N=22, Recruiting, Guangzhou Lupeng Pharmaceutical Company LTD. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    rocbrutinib (LP-168)
    over1year
    A Food Effect Study of LP-168 Tablets in Healthy Subjects (clinicaltrials.gov)
    P1, N=22, Not yet recruiting, Guangzhou Lupeng Pharmaceutical Company LTD.
    New P1 trial
    |
    rocbrutinib (LP-168)