Rabacfosadine

Rabacfosadine
Clinical data
Trade names	Tanovea
Other names	GS-9219
AHFS/Drugs.com	Veterinary Use
License data	US DailyMed: Rabacfosadine;
Routes of; administration	Intravenous
ATCvet code	QL01BB90 (WHO) ;
Legal status
Legal status	US: ℞-only;
Identifiers
CAS Number	859209-74-8;
PubChem CID	16047979;
DrugBank	DB12762;
ChemSpider	4486268;
UNII	M39BO43J9W;
KEGG	D10723;
ChEMBL	ChEMBL1823518;
CompTox Dashboard (EPA)	DTXSID10235245 ;
Chemical and physical data
Formula	C11H35N8O6P
Molar mass	406.425 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCOC( = O)[C@H](C)NP( = O)(COCCN1C = NC2 = C1N = C(N = C2NC3CC3)N)N[C@@H](C)C( = O)OCC;
	InChI 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 name Tanovea, is a guanine nucleotide analog used for the treatment of lymphoma in dogs.^[1] It was developed by Gilead 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 of apoptosis.^[3] It also inhibits the proliferation of lymphocytes in dogs with naturally occurring lymphoma.^[4]

Rabacfosadine was granted conditional approval by the US Food 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

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

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

^ ^a ^b "Tanovea- rabacfosadine succinate injection, powder, for solution". DailyMed. 17 January 2023. Retrieved 1 July 2024.
^ 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.
^ 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.
^ 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.
^ ^a ^b "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 from the original on 1 July 2017.
^ ^a ^b ^c ^d "FDA Grants First Full Approval for Treatment of Lymphoma in Dogs". U.S. Food and Drug Administration (FDA) (Press release). 15 July 2021. Retrieved 27 July 2021. This article incorporates text from this source, which is in the public domain.

[Tanovea_FDA_label-1] "Tanovea- rabacfosadine succinate injection, powder, for solution". DailyMed. 17 January 2023. Retrieved 1 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.

[:0-5] "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 from the original on 1 July 2017.

[FDA_PR-6] "FDA Grants First Full Approval for Treatment of Lymphoma in Dogs". U.S. Food and Drug Administration (FDA) (Press release). 15 July 2021. Retrieved 27 July 2021. This article incorporates text from this source, which is in the public domain.

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