ଫଲଭେଷ୍ଟ୍ରାଣ୍ଟ

ଫଲଭେଷ୍ଟ୍ରାଣ୍ଟ
Clinical data
Pronunciation	/fʊlˈvɛstrənt/; fuul-VES-trənt
Trade names	Faslodex, others
Synonyms	ICI-182780; ZD-182780; ZD-9238; 7α-[9-[(4,4,5,5,5-Pentafluoropentyl)-sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17β-diol
AHFS/Drugs.com	monograph
data	EU EMA: yes;
Pregnancy; category	AU: D ; D;
Routes of; administration	Intramuscular injection
Legal status
Legal status	AU: S4 (Prescription only) ; US: ℞-only ; EU: Rx-only ; ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	Low
Protein binding	99%
Metabolism	Hydroxylation, conjugation (glucuronidation, sulfation)
Elimination half-life	IM: 40–50 days
Identifiers
	IUPAC name (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol;
ECHA InfoCard	100.170.955
Chemical and physical data
Formula	C32H47F5O3S
Molar mass	୬୦୬.୭୮ g·mol−1
3D model (JSmol)	Interactive image;
	SMILES FC(F)(F)C(F)(F)CCCS(=O)CCCCCCCCCC3Cc1c(ccc(O)c1)[C@H]2CC[C@]4([C@H]([C@@H]23)CC[C@@H]4O)C;
	InChI InChI=1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,41?/m1/s1; Key:VWUXBMIQPBEWFH-WCCTWKNTSA-N;
(verify)

ଫଲଭେଷ୍ଟ୍ରାଣ୍ଟ, ଅନ୍ୟମାନଙ୍କ ମଧ୍ୟରେ ଏକ ବେପାର ନାମ ଫାସଲୋଡେକ୍ସ, ଏକ ଔଷଧ ଯାହା ସ୍ତନ କର୍କଟ ରୋଗର ଚିକିତ୍ସା ପାଇଁ ବ୍ୟବହୃତ ହୁଏ ।^[୨] ନିର୍ଦ୍ଦିଷ୍ଟ ଭାବରେ ଏହା ହରମୋନ୍ ରିସେପ୍ଟର (HR) ସକରାତ୍ମକ କ୍ଷେତ୍ରରେ ବ୍ୟବହୃତ ହୁଏ ।^[୩] ^[୪] ଏହା ମାଂସପେଶୀରେ ଇଞ୍ଜେକ୍ସନ ଆକାରରେ ଦିଆଯାଏ ।^[୨]

ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ବାନ୍ତି, ତରଳ ଝାଡ଼ା, ମୁଣ୍ଡବିନ୍ଧା, ଯନ୍ତ୍ରଣା, ଗରମ ଫ୍ଲସ, କାଶ, ଫୁଲା, ରାସ ଏବଂ ଶୋଇବାରେ ଅସୁବିଧା ହୋଇପାରେ ।^[୨] ଅନ୍ୟ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ସ୍ୱଳ୍ପ ଶ୍ୱେତ ରକ୍ତ କଣିକା, ସ୍ୱଳ୍ପ ଲୋହିତ ରକ୍ତ କଣିକା, ଥ୍ରୋମ୍ବୋସାଇଟିପେନିଆ, ସଂକ୍ରମଣ ଏବଂ ଯକୃତ ସମସ୍ୟା ହୋଇପାରେ ।^[୪] ଏହା ଗର୍ଭଧାରଣ କିମ୍ବା ସ୍ତନ୍ୟପାନର ସସମୟରେ ବ୍ୟବହାର କରାଯିବା ଉଚିତ୍ ନୁହେଁ ।^[୪] ଏହା ଏକ ସିଲେକ୍ଟିଭ୍ ଇଷ୍ଟ୍ରୋଜେନ୍ ରିସେପ୍ଟର ଡିଗ୍ରେଡର୍ (SERD) ଯାହା ଇଷ୍ଟ୍ରୋଜେନ୍ ରିସେପ୍ଟର ସହିତ ବାନ୍ଧନ ଯୁକ୍ତ ହୋଇ ସେମାନଙ୍କର ବିନାଶ କରାଏ ।^[୫]

୨୦୦୨ ମସିହାରେ ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଏବଂ ୨୦୦୪ରେ ୟୁରୋପରେ ଡାକ୍ତରୀ ବ୍ୟବହାର ପାଇଁ ଫଲଭେଷ୍ଟ୍ରାଣ୍ଟ ଅନୁମୋଦିତ ହୋଇଥିଲା ।^[୨] ^[୪] ଏହା ଏକ ସାଧାରଣ ଔଷଧ ଭାବରେ ଉପଲବ୍ଧ ।^[୬] ଯୁକ୍ତରାଜ୍ୟରେ ୨୦୨୧ରେ ଡୋଜ ପିଛା ୫୨୦ ପାଉଣ୍ଡ ଖର୍ଚ୍ଚ ହୁଏ ।^[୬]ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଏହି ରାଶିପରିମାଣର ମୁଲ୍ୟ ପ୍ରାୟ ୧୦୦ ଡଲାର ।^[୭]

ଆଧାର

↑ ^୧.୦ ^୧.୧ ^୧.୨ ^୧.୩ Dörwald FZ (4 February 2013). Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. John Wiley & Sons. pp. 486–. ISBN 978-3-527-64565-7. Archived from the original on 10 October 2021. Retrieved 19 September 2021.
↑ ^୨.୦ ^୨.୧ ^୨.୨ ^୨.୩ "Fulvestrant". The American Society of Health-System Pharmacists. Archived from the original on 2 February 2017. Retrieved 8 January 2021.
↑ "DailyMed - FULVESTRANT injection, solution". dailymed.nlm.nih.gov. Archived from the original on 12 December 2021. Retrieved 12 December 2021.
↑ ^୪.୦ ^୪.୧ ^୪.୨ ^୪.୩ "Faslodex". Archived from the original on 19 October 2021. Retrieved 12 December 2021.
↑ Lai AC, Crews CM (February 2017). "Induced protein degradation: an emerging drug discovery paradigm". Nature Reviews. Drug Discovery. 16 (2): 101–114. doi:10.1038/nrd.2016.211. PMC 5684876. PMID 27885283.
↑ ^୬.୦ ^୬.୧ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 996. ISBN 978-0857114105.
↑ "Faslodex Prices and Faslodex Coupons - GoodRx". GoodRx. Retrieved 12 December 2021.

[Dörwald2013-1] ୧.୦ ^୧.୧ ^୧.୨ ^୧.୩ Dörwald FZ (4 February 2013). Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. John Wiley & Sons. pp. 486–. ISBN 978-3-527-64565-7. Archived from the original on 10 October 2021. Retrieved 19 September 2021.

[AHFS2021-2] ୨.୦ ^୨.୧ ^୨.୨ ^୨.୩ "Fulvestrant". The American Society of Health-System Pharmacists. Archived from the original on 2 February 2017. Retrieved 8 January 2021.

[PI2021-3] "DailyMed - FULVESTRANT injection, solution". dailymed.nlm.nih.gov. Archived from the original on 12 December 2021. Retrieved 12 December 2021.

[EPAR2021-4] ୪.୦ ^୪.୧ ^୪.୨ ^୪.୩ "Faslodex". Archived from the original on 19 October 2021. Retrieved 12 December 2021.

[NRDD2016-5] Lai AC, Crews CM (February 2017). "Induced protein degradation: an emerging drug discovery paradigm". Nature Reviews. Drug Discovery. 16 (2): 101–114. doi:10.1038/nrd.2016.211. PMC 5684876. PMID 27885283.

[BNF81-6] ୬.୦ ^୬.୧ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 996. ISBN 978-0857114105.

[7] "Faslodex Prices and Faslodex Coupons - GoodRx". GoodRx. Retrieved 12 December 2021.

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Clinical data

Pronunciation	/fʊlˈvɛstrənt/ fuul-VES-trənt
Trade names	Faslodex, others
Synonyms	ICI-182780; ZD-182780; ZD-9238; 7α-[9-[(4,4,5,5,5-Pentafluoropentyl)-sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17β-diol
AHFS/Drugs.com	monograph
data	EU EMA: yes
Pregnancy category	AU: D D
Routes of administration	Intramuscular injection
Legal status
Legal status	AU: S4 (Prescription only) US: ℞-only EU: Rx-only ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	Low^[୧]
Protein binding	99%^[୧]
Metabolism	Hydroxylation, conjugation (glucuronidation, sulfation)^[୧]
Elimination half-life	IM: 40–50 days^[୧]
Identifiers
IUPAC name (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
ECHA InfoCard	100.170.955
Chemical and physical data
Formula	C₃₂H₄₇F₅O₃S
Molar mass	୬୦୬.୭୮ g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES FC(F)(F)C(F)(F)CCCS(=O)CCCCCCCCCC3Cc1c(ccc(O)c1)[C@H]2CC[C@]4([C@H]([C@@H]23)CC[C@@H]4O)C
InChI InChI=1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,41?/m1/s1 Key:VWUXBMIQPBEWFH-WCCTWKNTSA-N
(verify)