Pirtobrutinib

From Wikipedia, the free encyclopedia
(Redirected from Jaypirca)
Jump to navigation Jump to search

Pirtobrutinib
File:Pirtobrutinib.svg
Clinical data
Trade namesJaypirca
Other namesLOXO-305
AHFS/Drugs.comMonograph
MedlinePlusa623012
License data
Routes of
administration		By mouth
Drug classProtein kinase inhibitor
ATC code
Legal status
Legal status
Identifiers
  • 5-amino-3-(4-{[(5-fluoro-2-methoxybenzoyl)amino]methyl}phenyl)-1-((2S)-1,1,1-trifluoropropan-2-yl)pyrazole-4-carboxamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
E number{{#property:P628}}
CompTox Dashboard (EPA)
  • {{#property:P3117}}Lua error in Module:EditAtWikidata at line 29: attempt to index field 'wikibase' (a nil value).
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 29: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC22H21F4N5O3
Molar mass479.436 g·mol−1
3D model (JSmol)
  • COc1ccc(F)cc1C(=O)NCc1ccc(-c2nn([C@@H](C)C(F)(F)F)c(N)c2C(N)=O)cc1
  • InChI=1S/C22H21F4N5O3/c1-11(22(24,25)26)31-19(27)17(20(28)32)18(30-31)13-5-3-12(4-6-13)10-29-21(33)15-9-14(23)7-8-16(15)34-2/h3-9,11H,10,27H2,1-2H3,(H2,28,32)(H,29,33)/t11-/m0/s1
  • Key:FWZAWAUZXYCBKZ-NSHDSACASA-N

Pirtobrutinib, sold under the brand name Jaypirca, is an anti-cancer medication that is used to treat mantle cell lymphoma.[2][3][5] It inhibits B cell lymphocyte proliferation and survival by binding and inhibiting Bruton's tyrosine kinase (BTK).[6] It is taken by mouth.[2]

The most common adverse reactions include fatigue, musculoskeletal pain, diarrhea, edema, dyspnea, pneumonia, and bruising.[5][7] The most common adverse reactions when used to treat chronic lymphocytic leukemia or small lymphocytic leukemia include fatigue, bruising, cough, musculoskeletal pain, COVID-19, diarrhea, pneumonia, abdominal pain, dyspnea, hemorrhage, edema, nausea, pyrexia, and headache.[8]

Pirtobrutinib was approved for medical use in the United States in January 2023,[5][9][10][11] and in the European Union in November 2023.[3]

Medical uses

[edit | edit source]

In the United States, pirtobrutinib is indicated to treat relapsed or refractory mantle cell lymphoma after at least two lines of systemic therapy, including a Bruton's tyrosine kinase (BTK) inhibitor.[2][12] In December 2023, the US Food and Drug Administration (FDA) expanded the indication for pirtobrutinib to include the treatment of adults with chronic lymphocytic leukemia or small lymphocytic leukemia who have received at least two prior lines of therapy, including a BTK inhibitor and a BCL-2 inhibitor.[8][13] In December 2025, the FDA granted traditional approval for that indication.[14]

In the European Union, pirtobrutinib is indicated for the treatment of mantle cell lymphoma.[3]

Mechanism of action

[edit | edit source]

B cells are white cells of the lymphocyte subtype that produce antibodies, but when some of them grow uncontrollably they can be a cause of cancer. A key enzyme in B cell stimulation and survival is BTK, and pirtobrutinib inhibits BTK in a way that is different from the prototypical BTK inhibitor ibrutinib by binding in a different way that avoids a genetic change (mutation at active site cysteine residue C481 in BTK) that can make some tumors less responsive to ibrutinib.[6]

History

[edit | edit source]

Pirtobrutinib is manufactured by Eli Lilly and Company and was approved by the US Food and Drug Administration in January 2023, for the treatment of mantle cell lymphoma that has become refractory to other BTK inhibitors.[15]

Efficacy was evaluated in BRUIN (NCT03740529), an open-label, multicenter, single-arm trial of pirtobrutinib monotherapy that included 120 participants with mantle cell lymphoma previously treated with a Bruton's tyrosine kinase (BTK) inhibitor.[5] Participants had a median of three prior lines of therapy, with 93% having two or more prior lines.[5] The most common prior Bruton's tyrosine kinase inhibitors received were ibrutinib (67%), acalabrutinib (30%), and zanubrutinib (8%); 83% had discontinued their last Bruton's tyrosine kinase inhibitor due to refractory or progressive disease.[5] The trial was conducted at 49 sites in 10 countries in the United States, Europe, Australia, and Asia.[7] The same trial was used to assess safety and efficacy.[7]

Efficacy was evaluated in BRUIN (NCT03740529], an open-label, international, single-arm, multicohort trial that included 108 participants with chronic lymphocytic leukemia or small lymphocytic lymphoma previously treated with at least two prior lines of therapy, including a Bruton's tyrosine kinase (BTK) inhibitor and a B-cell lymphoma-2 (BCL-2) inhibitor.[8] Participants received a median of five prior lines of therapy (range: 2 to 11).[8] Seventy-seven percent of participants discontinued the last BTK inhibitor for refractory or progressive disease.[8] Pirtobrutinib was administered orally at 200 mg once daily and was continued until disease progression or unacceptable toxicity.[8]

Society and culture

[edit | edit source]
[edit | edit source]

In April 2023, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a conditional marketing authorization for the medicinal product Jaypirca, intended for the treatment of relapsed or refractory mantle cell lymphoma.[16] The applicant for this medicinal product is Eli Lilly Nederland B.V.[16] Pirtobrutinib was authorized for medical use in the European Union in November 2023.[3]

References

[edit | edit source]
  1. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  2. ^ a b c d Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  3. ^ a b c d e Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  4. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  5. ^ a b c d e f Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value). Error creating thumbnail: This article incorporates text from this source, which is in the public domain.
  6. ^ a b Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  7. ^ a b c Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  8. ^ a b c d e f Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value). Error creating thumbnail: This article incorporates text from this source, which is in the public domain.
  9. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  10. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  11. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  12. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  13. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  14. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  15. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  16. ^ a b Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value). Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

Further reading

[edit | edit source]
  • Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
[edit | edit source]
  • Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  • Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).

Lua error in mw.title.lua at line 392: bad argument #2 to 'title.new' (unrecognized namespace name 'Portal'). Lua error in Module:Authority_control at line 153: attempt to index field 'wikibase' (a nil value).

Retrieved from "http://70.231.62.181/index.php?title=Pirtobrutinib&oldid=16372650"