Prab at 21:02, 16 March 2025

2025-03-16T21:02:20Z

← Older revision		Revision as of 21:02, 16 March 2025
Line 49:		Line 49:

	{{Antineoplastic-drug-stub}}		{{Antineoplastic-drug-stub}}
	~~{{No image}}~~
	<gallery>		<gallery>
	File:Exisulind structure.svg\|Exisulind		File:Exisulind structure.svg\|Exisulind
	</gallery>		</gallery>

Prab: CSV import

2025-02-20T01:03:46Z

CSV import

← Older revision		Revision as of 01:03, 20 February 2025
Line 50:		Line 50:
	{{Antineoplastic-drug-stub}}		{{Antineoplastic-drug-stub}}
	{{No image}}		{{No image}}
			<gallery>
			File:Exisulind structure.svg\|Exisulind
			</gallery>

Prab: CSV import

2025-02-10T17:07:31Z

CSV import

← Older revision		Revision as of 17:07, 10 February 2025
Line 49:		Line 49:

	{{Antineoplastic-drug-stub}}		{{Antineoplastic-drug-stub}}
			{{No image}}

Prab: 1 revision imported

2019-09-01T19:37:57Z

1 revision imported

New page

{{Chembox
| ImageFile = Exisulind structure.svg
| ImageSize = 225px
| ImageAlt =
| IUPACName = 2-[(1''Z'')-5-fluoro-1-[(4-methanesulfonylphenyl)methylidene]-2-methyl-1''H''-inden-3-yl]acetic acid
| OtherNames = Sulindac sulfone, Aptosyn, FGN-1, Prevatac
|Section1={{Chembox Identifiers
| CASNo = 59973-80-7
| PubChem = 5472495
| ChemSpiderID = 4582441
| InChI = 1/C20H17FO4S/c1-12-17(9-13-3-6-15(7-4-13)26(2,24)25)16-8-5-14(21)10-19(16)18(12)11-20(22)23/h3-10H,11H2,1-2H3,(H,22,23)/b17-9-
| InChIKey = MVGSNCBCUWPVDA-MFOYZWKCBW
| StdInChI = 1S/C20H17FO4S/c1-12-17(9-13-3-6-15(7-4-13)26(2,24)25)16-8-5-14(21)10-19(16)18(12)11-20(22)23/h3-10H,11H2,1-2H3,(H,22,23)/b17-9-
| StdInChIKey = MVGSNCBCUWPVDA-MFOYZWKCSA-N
| RTECS =
| MeSHName =
| ChEBI = 64212
| ChEMBL = 488025
| SMILES = CC1=C(CC(O)=O)C2=C(C=CC(F)=C2)\C1=C/C1=CC=C(C=C1)S(C)(=O)=O }}
|Section2={{Chembox Properties
| Formula = C20H17FO4S
| MolarMass = 372.41 g/mol
| Appearance =
| Density =
| MeltingPt =
| BoilingPt =
| Solubility = }}
|Section3={{Chembox Hazards
| MainHazards =
| FlashPt =
| AutoignitionPt = }}
}}

'''Exisulind''' (tentative trade name '''Aptosyn''') is an [[antineoplastic]] agent. It acts by inhibiting the [[enzyme]] [[cGMP-specific phosphodiesterase type 5|cyclic guanosine monophosphate phosphodiesterase type 5]] ({{EC number|3.1.4.17}}).<ref>{{cite journal|last1=[No authors listed]|title=Exisulind: Aptosyn, FGN 1, Prevatac, sulindac sulfone.|journal=Drugs in R&D|date=2004|volume=5|issue=4|pages=220–6|pmid=15230629}}</ref> It is the sulfone derivative of [[sulindac]], an [[NSAID]]. Unlike sulindac, it has known effects on prostaglandin synthesis.<ref>{{cite journal|last1=van Stolk|first1=R|last2=Stoner|first2=G|last3=Hayton|first3=WL|last4=Chan|first4=K|last5=DeYoung|first5=B|last6=Kresty|first6=L|last7=Kemmenoe|first7=BH|last8=Elson|first8=P|last9=Rybicki|first9=L|last10=Church|first10=J|last11=Provencher|first11=K|last12=McLain|first12=D|last13=Hawk|first13=E|last14=Fryer|first14=B|last15=Kelloff|first15=G|last16=Ganapathi|first16=R|last17=Budd|first17=GT|title=Phase I trial of Exisulind (Sulindac Sulfone, FGN-1) as a chemopreventive agent in patients with familial adenomatous polyposis.|journal=Clinical Cancer Research|date=January 2000|volume=6|issue=1|pages=78–89|pmid=10656435}}</ref> It was developed as the potential treatment of several conditions including [[familial adenomatous polyposis]] (FAP), precancerous sporadic [[Colorectal polyp|colonic polyps]], [[Cervical intraepithelial neoplasia|cervical dysplasia]] and the prevention of tumor recurrence in [[prostate cancer|prostate]] and [[breast cancer]].<ref>{{cite journal|last1=Griffiths|first1=GJ|title=Exisulind Cell Pathways.|journal=Current Opinion in Investigational Drugs|date=November 2000|volume=1|issue=3|pages=386–91|pmid=11249724}}</ref> Exisulind inhibits the enzyme [[cGMP-specific phosphodiesterase type 5|cGMP-PDE]], overexpressed in precancerous and cancerous colorectal cells, and induces apoptosis in such cells with minimal effects on normal cells. This apoptotic effect is independent of [[PTGS1|COX-1]] or [[Prostaglandin-endoperoxide synthase 2|COX-2]] inhibition, [[p53]], [[Bcl-2]], or [[cell cycle]] arrest. Preclinical evidence suggests that exisulind also inhibits [[angiogenesis]].<ref>{{cite journal|last1=Skopińska-Rózewska|first1=E|last2=Piazza|first2=GA|last3=Sommer|first3=E|last4=Pamukcu|first4=R|last5=Barcz|first5=E|last6=Filewska|first6=M|last7=Kupis|first7=W|last8=Caban|first8=R|last9=Rudziński|first9=P|last10=Bogdan|first10=J|last11=Mlekodaj|first11=S|last12=Sikorska|first12=E|title=Inhibition of Angiogenesis by Sulindac and its Sulfone Metabolite (FGN-1): a Potential Mechanism for Their Antineoplastic Properties.|journal=International Journal of Tissue Reactions|date=1998|volume=20|issue=3|pages=85–9|pmid=9894180}}</ref>

== See also ==
* [[Sulindac]]

{{Intracellular chemotherapeutic agents}}

==References==
{{Reflist}}

[[Category:Antineoplastic drugs]]
[[Category:Benzosulfones]]
[[Category:Carboxylic acids]]
[[Category:Indenes]]

{{Antineoplastic-drug-stub}}

Exisulind - Revision history

Prab at 21:02, 16 March 2025

Prab: CSV import

Prab: CSV import

Prab: 1 revision imported