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2021 5
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2024 15

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Pirtobrutinib in relapsed or refractory B-cell malignancies (BRUIN): a phase 1/2 study.
Mato AR, Shah NN, Jurczak W, Cheah CY, Pagel JM, Woyach JA, Fakhri B, Eyre TA, Lamanna N, Patel MR, Alencar A, Lech-Maranda E, Wierda WG, Coombs CC, Gerson JN, Ghia P, Le Gouill S, Lewis DJ, Sundaram S, Cohen JB, Flinn IW, Tam CS, Barve MA, Kuss B, Taylor J, Abdel-Wahab O, Schuster SJ, Palomba ML, Lewis KL, Roeker LE, Davids MS, Tan XN, Fenske TS, Wallin J, Tsai DE, Ku NC, Zhu E, Chen J, Yin M, Nair B, Ebata K, Marella N, Brown JR, Wang M. Mato AR, et al. Lancet. 2021 Mar 6;397(10277):892-901. doi: 10.1016/S0140-6736(21)00224-5. Lancet. 2021. PMID: 33676628 Clinical Trial.
The most common adverse event of grade 3 or higher was neutropenia (32 [10%]). There was no correlation between pirtobrutinib exposure and the frequency of grade 3 treatment-related adverse events. ...Pirtobrutinib might address a growing unmet need for alternative …
The most common adverse event of grade 3 or higher was neutropenia (32 [10%]). There was no correlation between pirtobrutinib exposur …
Pirtobrutinib after a Covalent BTK Inhibitor in Chronic Lymphocytic Leukemia.
Mato AR, Woyach JA, Brown JR, Ghia P, Patel K, Eyre TA, Munir T, Lech-Maranda E, Lamanna N, Tam CS, Shah NN, Coombs CC, Ujjani CS, Fakhri B, Cheah CY, Patel MR, Alencar AJ, Cohen JB, Gerson JN, Flinn IW, Ma S, Jagadeesh D, Rhodes JM, Hernandez-Ilizaliturri F, Zinzani PL, Seymour JF, Balbas M, Nair B, Abada P, Wang C, Ruppert AS, Wang D, Tsai DE, Wierda WG, Jurczak W. Mato AR, et al. N Engl J Med. 2023 Jul 6;389(1):33-44. doi: 10.1056/NEJMoa2300696. N Engl J Med. 2023. PMID: 37407001 Clinical Trial.
BACKGROUND: Patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) have poor outcomes after the failure of covalent Bruton's tyrosine kinase (BTK) inhibitor treatment, and new therapeutic options are needed. Pirtobrutinib, a highly sele …
BACKGROUND: Patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) have poor outcomes after the failure of cov …
Pirtobrutinib in Covalent Bruton Tyrosine Kinase Inhibitor Pretreated Mantle-Cell Lymphoma.
Wang ML, Jurczak W, Zinzani PL, Eyre TA, Cheah CY, Ujjani CS, Koh Y, Izutsu K, Gerson JN, Flinn I, Tessoulin B, Alencar AJ, Ma S, Lewis D, Lech-Maranda E, Rhodes J, Patel K, Maddocks K, Lamanna N, Wang Y, Tam CS, Munir T, Nagai H, Hernandez-Ilizaliturri F, Kumar A, Fenske TS, Seymour JF, Zelenetz AD, Nair B, Tsai DE, Balbas M, Walgren RA, Abada P, Wang C, Zhao J, Mato AR, Shah NN. Wang ML, et al. J Clin Oncol. 2023 Aug 20;41(24):3988-3997. doi: 10.1200/JCO.23.00562. Epub 2023 May 16. J Clin Oncol. 2023. PMID: 37192437 Free PMC article.
PURPOSE: Pirtobrutinib is a highly selective, noncovalent (reversible) Bruton tyrosine kinase inhibitor (BTKi). ...Pirtobrutinib was well tolerated with low rates of treatment discontinuation because of toxicity....
PURPOSE: Pirtobrutinib is a highly selective, noncovalent (reversible) Bruton tyrosine kinase inhibitor (BTKi). ...Pirtobrutinib …
Pirtobrutinib: First Approval.
Keam SJ. Keam SJ. Drugs. 2023 Apr;83(6):547-553. doi: 10.1007/s40265-023-01860-1. Drugs. 2023. PMID: 37004673 Review.
Pirtobrutinib (Jaypirca(TM)), a highly selective, non-covalent, reversible Bruton's tyrosine kinase (BTK) inhibitor, is being developed by Eli Lilly and Company (Lilly) for the treatment of B-cell leukemias and lymphomas. ...This article summarizes the milestones in the de …
Pirtobrutinib (Jaypirca(TM)), a highly selective, non-covalent, reversible Bruton's tyrosine kinase (BTK) inhibitor, is being develop …
Preclinical characterization of pirtobrutinib, a highly selective, noncovalent (reversible) BTK inhibitor.
Gomez EB, Ebata K, Randeria HS, Rosendahl MS, Cedervall EP, Morales TH, Hanson LM, Brown NE, Gong X, Stephens J, Wu W, Lippincott I, Ku KS, Walgren RA, Abada PB, Ballard JA, Allerston CK, Brandhuber BJ. Gomez EB, et al. Blood. 2023 Jul 6;142(1):62-72. doi: 10.1182/blood.2022018674. Blood. 2023. PMID: 36796019 Free PMC article.
Pirtobrutinib, but not cBTKis, prevented Y551 phosphorylation in the activation loop. ...Enzymatic profiling showed that pirtobrutinib was highly selective for BTK in >98% of the human kinome, and in follow-up cellular studies pirtobrutinib retained >10 …
Pirtobrutinib, but not cBTKis, prevented Y551 phosphorylation in the activation loop. ...Enzymatic profiling showed that pirtobrut …
Diagnosis and Treatment of Chronic Lymphocytic Leukemia: A Review.
Shadman M. Shadman M. JAMA. 2023 Mar 21;329(11):918-932. doi: 10.1001/jama.2023.1946. JAMA. 2023. PMID: 36943212 Review.
Highly effective novel targeted agents include BTK inhibitors such as acalabrutinib, zanubrutinib, ibrutinib, and pirtobrutinib or BCL2 inhibitors such as venetoclax....
Highly effective novel targeted agents include BTK inhibitors such as acalabrutinib, zanubrutinib, ibrutinib, and pirtobrutinib or BC …
Pirtobrutinib targets BTK C481S in ibrutinib-resistant CLL but second-site BTK mutations lead to resistance.
Naeem A, Utro F, Wang Q, Cha J, Vihinen M, Martindale S, Zhou Y, Ren Y, Tyekucheva S, Kim AS, Fernandes SM, Saksena G, Rhrissorrakrai K, Levovitz C, Danysh BP, Slowik K, Jacobs RA, Davids MS, Lederer JA, Zain R, Smith CIE, Leshchiner I, Parida L, Getz G, Brown JR. Naeem A, et al. Blood Adv. 2023 May 9;7(9):1929-1943. doi: 10.1182/bloodadvances.2022008447. Blood Adv. 2023. PMID: 36287227 Free PMC article.
We demonstrate that primary CLL cells from responding patients on the pirtobrutinib trial show reduced BCR signaling, cell survival, and CCL3/CCL4 chemokine secretion. At time of progression, these primary CLL cells show increasing resistance to pirtobrutinib in sig …
We demonstrate that primary CLL cells from responding patients on the pirtobrutinib trial show reduced BCR signaling, cell survival, …
Treatment of Richter's syndrome.
Thompson PA, Siddiqi T. Thompson PA, et al. Hematology Am Soc Hematol Educ Program. 2022 Dec 9;2022(1):329-336. doi: 10.1182/hematology.2022000345. Hematology Am Soc Hematol Educ Program. 2022. PMID: 36485138 Free PMC article. Review.
The BCL2 inhibitor venetoclax in combination with R-EPOCH CIT achieved CR in 50% of patients, and a study of venetoclax-R-CHOP is ongoing. The noncovalent Bruton's tyrosine kinase inhibitor pirtobrutinib has achieved responses in approximately two-thirds of heavily pretrea …
The BCL2 inhibitor venetoclax in combination with R-EPOCH CIT achieved CR in 50% of patients, and a study of venetoclax-R-CHOP is ongoing. T …
Resistance to Bruton tyrosine kinase inhibition in chronic lymphocytic leukaemia and non-Hodgkin lymphoma.
Nakhoda S, Vistarop A, Wang YL. Nakhoda S, et al. Br J Haematol. 2023 Jan;200(2):137-149. doi: 10.1111/bjh.18418. Epub 2022 Aug 27. Br J Haematol. 2023. PMID: 36029036 Free PMC article. Review.
Bruton tyrosine kinase inhibitors (BTKi) have transformed the therapeutic landscape of chronic lymphocytic leukaemia (CLL) and non-Hodgkin lymphoma. ...We incorporate the most recent findings regarding mechanisms of resistance to covalent and non-covalent inhibitors, inclu …
Bruton tyrosine kinase inhibitors (BTKi) have transformed the therapeutic landscape of chronic lymphocytic leukaemia (CLL) and non-Ho …
Enrichment of BTK Leu528Trp mutations in patients with CLL on zanubrutinib: potential for pirtobrutinib cross-resistance.
Blombery P, Thompson ER, Lew TE, Tiong IS, Bennett R, Cheah CY, Lewis KL, Handunnetti SM, Tang CPS, Roberts A, Seymour JF, Tam CS. Blombery P, et al. Blood Adv. 2022 Oct 25;6(20):5589-5592. doi: 10.1182/bloodadvances.2022008325. Blood Adv. 2022. PMID: 35901282 Free PMC article.
We describe 2 patients with BTK Leu528Trp mutations who showed clinical cross-resistance and progressive enrichment of the BTK Leu528Trp mutation over time when treated with the noncovalent BTKi pirtobrutinib. Both patients subsequently responded to venetoclax-based treatm …
We describe 2 patients with BTK Leu528Trp mutations who showed clinical cross-resistance and progressive enrichment of the BTK Leu528Trp mut …
48 results