Difference between revisions of "Pirtobrutinib (Jaypirca)"
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From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/btk-inhibitor-loxo-305 NCI Drug Dictionary]: An orally available, selective, non-covalent Bruton’s tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Upon oral administration, BTK inhibitor LOXO-305 selectively and reversibly binds to BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, thereby inhibiting the growth of malignant B cells that overexpress BTK. Reversible binding of LOXO-305 may preserve antitumor activity in the presence of certain acquired resistance mutations, including C481 mutated BTK, and limit toxicity associated with inhibition of other non-BTK kinases. | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/btk-inhibitor-loxo-305 NCI Drug Dictionary]: An orally available, selective, non-covalent Bruton’s tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Upon oral administration, BTK inhibitor LOXO-305 selectively and reversibly binds to BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, thereby inhibiting the growth of malignant B cells that overexpress BTK. Reversible binding of LOXO-305 may preserve antitumor activity in the presence of certain acquired resistance mutations, including C481 mutated BTK, and limit toxicity associated with inhibition of other non-BTK kinases. | ||
| − | == | + | ==Diseases for which it is used== |
| + | *[[Mantle cell lymphoma]] | ||
#'''BRUIN:''' [https://doi.org/10.1016/S0140-6736(21)00224-5 link to original article] NCT03740529 | #'''BRUIN:''' [https://doi.org/10.1016/S0140-6736(21)00224-5 link to original article] NCT03740529 | ||
==Mechanisms of resistance== | ==Mechanisms of resistance== | ||
#Wang E, Mi X, Thompson MC, Montoya S, Notti RQ, Afaghani J, Durham BH, Penson A, Witkowski MT, Lu SX, Bourcier J, Hogg SJ, Erickson C, Cui D, Cho H, Singer M, Totiger TM, Chaudhry S, Geyer M, Alencar A, Linley AJ, Palomba ML, Coombs CC, Park JH, Zelenetz A, Roeker L, Rosendahl M, Tsai DE, Ebata K, Brandhuber B, Hyman DM, Aifantis I, Mato A, Taylor J, Abdel-Wahab O. Mechanisms of Resistance to Noncovalent Bruton's Tyrosine Kinase Inhibitors. N Engl J Med. 2022 Feb 24;386(8):735-743. [https://doi.org/10.1056/nejmoa2114110 link to original article] [https://pubmed.ncbi.nlm.nih.gov/35196427/ PubMed] | #Wang E, Mi X, Thompson MC, Montoya S, Notti RQ, Afaghani J, Durham BH, Penson A, Witkowski MT, Lu SX, Bourcier J, Hogg SJ, Erickson C, Cui D, Cho H, Singer M, Totiger TM, Chaudhry S, Geyer M, Alencar A, Linley AJ, Palomba ML, Coombs CC, Park JH, Zelenetz A, Roeker L, Rosendahl M, Tsai DE, Ebata K, Brandhuber B, Hyman DM, Aifantis I, Mato A, Taylor J, Abdel-Wahab O. Mechanisms of Resistance to Noncovalent Bruton's Tyrosine Kinase Inhibitors. N Engl J Med. 2022 Feb 24;386(8):735-743. [https://doi.org/10.1056/nejmoa2114110 link to original article] [https://pubmed.ncbi.nlm.nih.gov/35196427/ PubMed] | ||
| + | |||
| + | ==History of changes in FDA indication== | ||
| + | *1/27/2023: Granted accelerated approval for relapsed or refractory [[Mantle cell lymphoma|mantle cell lymphoma (MCL)]] after at least two lines of systemic therapy, including a BTK inhibitor. ''(Based on BRUIN)'' | ||
==Also known as== | ==Also known as== | ||
*'''Code name:''' LOXO-305 | *'''Code name:''' LOXO-305 | ||
| + | *'''Brand name:''' Jaypirca | ||
[[Category:Drugs]] | [[Category:Drugs]] | ||
[[Category:Oral medications]] | [[Category:Oral medications]] | ||
[[Category:BTK inhibitors]] | [[Category:BTK inhibitors]] | ||
| − | [[Category: | + | [[Category:Mantle cell lymphoma medications]] |
| + | [[Category:FDA approved in 2023]] | ||
Revision as of 16:31, 28 January 2023
Mechanism of action
From the NCI Drug Dictionary: An orally available, selective, non-covalent Bruton’s tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Upon oral administration, BTK inhibitor LOXO-305 selectively and reversibly binds to BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, thereby inhibiting the growth of malignant B cells that overexpress BTK. Reversible binding of LOXO-305 may preserve antitumor activity in the presence of certain acquired resistance mutations, including C481 mutated BTK, and limit toxicity associated with inhibition of other non-BTK kinases.
Diseases for which it is used
- BRUIN: link to original article NCT03740529
Mechanisms of resistance
- Wang E, Mi X, Thompson MC, Montoya S, Notti RQ, Afaghani J, Durham BH, Penson A, Witkowski MT, Lu SX, Bourcier J, Hogg SJ, Erickson C, Cui D, Cho H, Singer M, Totiger TM, Chaudhry S, Geyer M, Alencar A, Linley AJ, Palomba ML, Coombs CC, Park JH, Zelenetz A, Roeker L, Rosendahl M, Tsai DE, Ebata K, Brandhuber B, Hyman DM, Aifantis I, Mato A, Taylor J, Abdel-Wahab O. Mechanisms of Resistance to Noncovalent Bruton's Tyrosine Kinase Inhibitors. N Engl J Med. 2022 Feb 24;386(8):735-743. link to original article PubMed
History of changes in FDA indication
- 1/27/2023: Granted accelerated approval for relapsed or refractory mantle cell lymphoma (MCL) after at least two lines of systemic therapy, including a BTK inhibitor. (Based on BRUIN)
Also known as
- Code name: LOXO-305
- Brand name: Jaypirca