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Rabacfosadine

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Chemical compound

Pharmaceutical compound
Rabacfosadine
Clinical data
Trade namesTanovea
Other namesGS-9219
AHFS/Drugs.comVeterinary Use
License data
Routes of
administration
Intravenous
ATCvet code
Legal status
Legal status
Identifiers
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC11H35N8O6P
Molar mass406.425 g·mol−1
3D model (JSmol)
  • CCOC( = O)[C@H](C)NP( = O)(COCCN1C = NC2 = C1N = C(N = C2NC3CC3)N)N[C@@H](C)C( = O)OCC
  • InChI=1S/C21H35N8O6P/c1-5-34-19(30)13(3)27-36(32,28-14(4)20(31)35-6-2)12-33-10-9-29-11-23-16-17(24-15-7-8-15)25-21(22)26-18(16)29/h11,13-15H,5-10,12H2,1-4H3,(H2,27,28,32)(H3,22,24,25,26)/t13-,14-/m0/s1
  • Key:ANSPEDQTHURSFQ-KBPBESRZSA-N

Rabacfosadine, sold under the brand nameTanovea, is aguaninenucleotide analog used for the treatment oflymphoma in dogs.[1] It was developed byGilead Sciences as GS-9219.[2]

The active form of rabacfosadine is a chain-terminating inhibitor of the major deoxyribonucleic acid (DNA) polymerases.In vitro studies have demonstrated that rabacfosadine inhibits DNA synthesis, resulting in S phase arrest and induction ofapoptosis.[3] It also inhibits the proliferation of lymphocytes in dogs with naturally occurring lymphoma.[4]

Rabacfosadine was granted conditional approval by the USFood and Drug Administration (FDA) in December 2016,[5] and became the first medication to receive full approval for the treatment of canine lymphoma in July 2021.[6]

Veterinary uses

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In July 2021, the U.S.Food and Drug Administration (FDA) approved Tanovea to treat lymphoma in dogs.[6] Lymphoma, also called lymphosarcoma, is a type of cancer that can affect many species, including dogs.[6] Rabacfosadine is the first conditionally approved new animal drug for dogs to achieve the FDA's full approval.[6]

Adverse effects

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Common side effects of rabacfosadine are decreased white blood cell count, diarrhea, vomiting, decreased appetite or loss of appetite, weight loss, decreased activity level, and skin problems. Other side effects may occur.[5]

References

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  1. ^ab"Tanovea- rabacfosadine succinate injection, powder, for solution".DailyMed. 17 January 2023. Retrieved1 July 2024.
  2. ^De Clercq E (August 2018)."Tanovea for the treatment of lymphoma in dogs".Biochemical Pharmacology.154:265–269.doi:10.1016/j.bcp.2018.05.010.PMID 29778492.
  3. ^Reiser H, Wang J, Chong L, Watkins WJ, Ray AS, Shibata R, et al. (May 2008)."GS-9219--a novel acyclic nucleotide analogue with potent antineoplastic activity in dogs with spontaneous non-Hodgkin's lymphoma".Clinical Cancer Research.14 (9):2824–32.doi:10.1158/1078-0432.CCR-07-2061.PMID 18451250.
  4. ^Lawrence J, Vanderhoek M, Barbee D, Jeraj R, Tumas DB, Vail DM (2009). "Use of 3'-deoxy-3'-[18F]fluorothymidine PET/CT for evaluating response to cytotoxic chemotherapy in dogs with non-Hodgkin's lymphoma".Veterinary Radiology & Ultrasound.50 (6):660–8.doi:10.1111/j.1740-8261.2009.01612.x.PMID 19999354.
  5. ^ab"FDA Conditionally Approves Tanovea-CA1, the first New Animal Drug for Treating Lymphoma in Dogs".U.S.Food and Drug Administration (FDA) (Press release). 3 January 2017. Archived fromthe original on 1 July 2017.
  6. ^abcd"FDA Grants First Full Approval for Treatment of Lymphoma in Dogs".U.S.Food and Drug Administration (FDA) (Press release). 15 July 2021. Archived fromthe original on 15 July 2021. Retrieved27 July 2021.Public Domain This article incorporates text from this source, which is in thepublic domain.
SPs/MIs
(M phase)
Blockmicrotubule assembly
Block microtubule disassembly
DNA replication
inhibitor
DNA precursors/
antimetabolites
(S phase)
Folic acid
Purine
Pyrimidine
Deoxyribonucleotide
Topoisomerase inhibitors
(S phase)
I
II
II+Intercalation
Crosslinking of DNA
(CCNS)
Alkylating
Platinum-based
Nonclassical
Intercalation
Photosensitizers/PDT
Other
Enzyme inhibitors
Receptor antagonists
Other/ungrouped
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