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Peer-reviewedCC BY-NC-ND 4.0Blood Cancer Journal

Bosmolisib (BR101801), a novel PI3K-δ/γ and DNA-PK inhibitor for relapsed/refractory patients with peripheral T-cell lymphoma: a phase I study

  • Tae Min Kim1
  • Seok Jin Kim2
  • Jin Seok Kim3
  • Deok-Hwan Yang4
  • Dok Hyun Yoon5
  • Won Sik Lee6
  • Eunyoung Lee7
  • Jeong-Ok Lee8
  • Ahmad Hatem Mattour9
  • Jorge Chaves10
  • Bong-Seog Kim11
11 affiliations
  1. 1Department of Internal Medicine, Seoul National University Hospital, Seoul National University College of Medicine, Seoul, Republic of Korea
  2. 2Division of Hematology-Oncology, Department of Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, Republic of Korea
  3. 3Division of Hematology, Department of Internal Medicine, Yonsei University College of Medicine, Severance Hospital, Seoul, Republic of Korea
  4. 4Hematology-Oncology, Chonnam National University Hwasun Hospital, Chonnam National Medical School, Gwangju, Republic of Korea
  5. 5Department of Oncology, Asan Medical Center, University of Ulsan College of Medicine, Seoul, Republic of Korea
  6. 6Department of Internal Medicine, Hemato-Oncology, Inje University Busan Paik Hospital, Busan, Republic of Korea
  7. 7Center for Hematologic Malignancy, National Cancer Center, Goyang, Republic of Korea
  8. 8Department of Internal Medicine, Seoul National University Bundang Hospital, Seoul National University College of Medicine, Seongnam, Republic of Korea
  9. 9Henry Ford Health System, Detroit, MI USA
  10. 10Northwest Medical Specialties, Tacoma, WA USA
  11. 11Research and Development Center, Boryung Company Limited, Seoul, Republic of Korea
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Abstract

Bosmolisib is a novel triple inhibitor of PI3K-δ/γ and DNA-PK for malignancy treatment. This was a first-in-human, phase 1, open-label, dose-escalation, and dose-expansion trial with relapsed/refractory (R/R) non-Hodgkin lymphoma (NHL). Patients received bosmolisib orally once daily in 28-day cycles across four dose levels (50–325 mg) until disease progression or unacceptable toxicity. The study utilized a 3 + 3 dose-escalation design to determine the maximum tolerated dose (MTD) and recommended phase 2 dose (RP2D), followed by expansion at RP2D. Primary endpoints were safety and MTD/RP2D determination; secondary endpoints included efficacy, pharmacokinetics, and pharmacodynamics. A total of 26 patients were enrolled in dose-escalation (N = 12) and dose-expansion (N = 14). Median age was 65 years with a median of 3 prior therapies. Bosmolisib demonstrated acceptable tolerability; dose-limiting toxicities were observed at 325 mg (alanine transaminase [ALT] increased and erythema multiforme), establishing MTD/RP2D at 200 mg. Most adverse events (AEs) were Grade 1–2, with the most common Grade ≥3 AEs (ALT 23.1%, aspartate transaminase 15.4%). Of 23 evaluable patients, the overall response rate (ORR) was 26.1%, and in PTCL patients, ORR was 31.6% with one patient achieving a durable complete response. Pharmacodynamics profiling showed statistically significant decrease in regulatory T-cells. These findings support evaluation of bosmolisib in a phase 2 trial (ClinicalTrials.gov number, NCT04018248).

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Cite

BibTeXRIS
BibTeX
@article{kim2026bosmolisib,
  title = {{Bosmolisib (BR101801), a novel PI3K-δ/γ and DNA-PK inhibitor for relapsed/refractory patients with peripheral T-cell lymphoma: a phase I study}},
  author = {Tae Min Kim and Seok Jin Kim and Jin Seok Kim and Deok-Hwan Yang and Dok Hyun Yoon and Won Sik Lee and Eunyoung Lee and Jeong-Ok Lee and Ahmad Hatem Mattour and Jorge Chaves and Bong-Seog Kim},
  journal = {Blood Cancer Journal},
  year = {2026},
  month = aug,
  doi = {10.1038/s41408-026-01600-0},
  url = {https://doi.org/10.1038/s41408-026-01600-0},
  note = {CC BY-NC-ND 4.0},
}
RIS
TY  - JOUR
TI  - Bosmolisib (BR101801), a novel PI3K-δ/γ and DNA-PK inhibitor for relapsed/refractory patients with peripheral T-cell lymphoma: a phase I study
AU  - Tae Min Kim
AU  - Seok Jin Kim
AU  - Jin Seok Kim
AU  - Deok-Hwan Yang
AU  - Dok Hyun Yoon
AU  - Won Sik Lee
AU  - Eunyoung Lee
AU  - Jeong-Ok Lee
AU  - Ahmad Hatem Mattour
AU  - Jorge Chaves
AU  - Bong-Seog Kim
PY  - 2026
DA  - 2026/08/07
JO  - Blood Cancer Journal
DO  - 10.1038/s41408-026-01600-0
UR  - https://doi.org/10.1038/s41408-026-01600-0
AB  - Bosmolisib is a novel triple inhibitor of PI3K-δ/γ and DNA-PK for malignancy treatment. This was a first-in-human, phase 1, open-label, dose-escalation, and dose-expansion trial with relapsed/refractory (R/R) non-Hodgkin lymphoma (NHL). Patients received bosmolisib orally once daily in 28-day cycles across four dose levels (50–325 mg) until disease progression or unacceptable toxicity. The study utilized a 3 + 3 dose-escalation design to determine the maximum tolerated dose (MTD) and recommended phase 2 dose (RP2D), followed by expansion at RP2D. Primary endpoints were safety and MTD/RP2D determination; secondary endpoints included efficacy, pharmacokinetics, and pharmacodynamics. A total of 26 patients were enrolled in dose-escalation (N = 12) and dose-expansion (N = 14). Median age was 65 years with a median of 3 prior therapies. Bosmolisib demonstrated acceptable tolerability; dose-limiting toxicities were observed at 325 mg (alanine transaminase [ALT] increased and erythema multiforme), establishing MTD/RP2D at 200 mg. Most adverse events (AEs) were Grade 1–2, with the most common Grade ≥3 AEs (ALT 23.1%, aspartate transaminase 15.4%). Of 23 evaluable patients, the overall response rate (ORR) was 26.1%, and in PTCL patients, ORR was 31.6% with one patient achieving a durable complete response. Pharmacodynamics profiling showed statistically significant decrease in regulatory T-cells. These findings support evaluation of bosmolisib in a phase 2 trial (ClinicalTrials.gov number, NCT04018248).
SN  - 2044-5385
ER  -