ଆପାଲୁଟାମାଇଡ

ଆପାଲୁଟାମାଇଡ
Clinical data
Trade names	Erleada, others
Synonyms	ARN-509; JNJ-56021927; JNJ-927; A52
AHFS/Drugs.com	monograph
MedlinePlus	a618018
data	US DailyMed: Erleada;
Pregnancy; category	AU: D ; US: N (Not classified yet) ; ;
Routes of; administration	By mouth
Legal status
Legal status	AU: S4 (Prescription only) ; UK: POM (Prescription only) ; US: ℞-only ; EU: Rx-only ; ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	100%
Protein binding	Apalutamide: 96%; NDMA: 95%
Metabolism	Liver (CYP2C8, CYP3A4)
Metabolites	• NDMA
Elimination half-life	Apalutamide: 3–4 days (at steady-state)
Excretion	Urine: 65%; Feces: 24%
Identifiers
	IUPAC name 4-[7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide;
ECHA InfoCard	100.235.115
Chemical and physical data
Formula	C21H15F4N5O2S
Molar mass	୪୭୭.୪୪ g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CNC(=O)C1=C(C=C(C=C1)N2C(=S)N(C(=O)C23CCC3)C4=CN=C(C(=C4)C(F)(F)F)C#N)F;
	InChI InChI=1S/C21H15F4N5O2S/c1-27-17(31)13-4-3-11(8-15(13)22)30-19(33)29(18(32)20(30)5-2-6-20)12-7-14(21(23,24)25)16(9-26)28-10-12/h3-4,7-8,10H,2,5-6H2,1H3,(H,27,31); Key:HJBWBFZLDZWPHF-UHFFFAOYSA-N;

ଆପାଲୁଟାମାଇଡ, ଅନ୍ୟମାନଙ୍କ ମଧ୍ୟରେ ଏକ ବେପାର ନାମ ଏର୍ଲେଡା ହେଉଛି ପ୍ରୋଷ୍ଟେଟ୍ କର୍କଟ୍ଟ ରୋଗର ଚିକିତ୍ସା ପାଇଁ ବ୍ୟବହୃତ ଏକ ଔଷଧ । ^[୨] ନିର୍ଦ୍ଦିଷ୍ଟ ଭାବରେ ଏହା ମେଟାଷ୍ଟାଟିକ୍ କାଷ୍ଟ୍ରେସନ୍-ସମ୍ବେଦନଶୀଳ ପ୍ରୋଷ୍ଟେଟ୍ କର୍କଟ ଏବଂ ଅଣ-ମେଟାଷ୍ଟାଟିକ୍ କାଷ୍ଟ୍ରେସନ୍-ପ୍ରତିରୋଧକ ପ୍ରୋଷ୍ଟେଟ୍ କର୍କଟ (NM-CRPC)ରେ ବ୍ୟବହୃତ ହୁଏ । ^[୨] ଏହା ପାଟିରେ ଦିଆଯାଏ । ^[୨]

ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ଥକ୍କାପଣ, ଗଣ୍ଠି ଯନ୍ତ୍ରଣା, ରାସ, ଦୁର୍ଗଟଣା ପତନ, ଉଚ୍ଚ ରକ୍ତଚାପ, ଗରମ ଫ୍ଲାସ୍ (hot flashes), ତରଳ ଝାଡ଼ା ଏବଂ ହାଡ ଭଙ୍ଗା ହୋଇପାରେ । ^[୨] ଅନ୍ୟ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ଷ୍ଟ୍ରୋକ ଏବଂ ବାତ ହୋଇପାରେ । ^[୨] ଗର୍ଭବତୀ ମହିଳାଙ୍କର ସ୍ୱାମୀମାନଙ୍କର ଓଷଧ ବ୍ୟବହାର ଯୋଗୁ ଶିଶୁର କ୍ଷତି ହୋଇପାରେ । ^[୨] ଏହା ଏକ ନନ୍ ଷ୍ଟେରଏଡାଲ୍ ଆଣ୍ଟିଆଣ୍ଡ୍ରୋଜେନ୍ (NSAA) ଏବଂ ଟେଷ୍ଟୋଷ୍ଟେରନ୍ ସହିତ ଆଣ୍ଡ୍ରୋଜେନମାନଙ୍କୁ ଅବରୋଧ କରି କାର୍ଯ୍ୟକ୍ଷମ ହୋଇଥାଏ । ^[୩] ^[୫] ଯେହେତୁ ପ୍ରୋଷ୍ଟେଟ କର୍କଟ ଆଣ୍ଡ୍ରୋଜେନ ଆବଶ୍ୟକ କରେ, ସେମାନଙ୍କୁ ଅବରୋଧ କରିବା ଏହାର ଅଭିବୃଦ୍ଧିକୁ ମନ୍ଥର କରିଥାଏ । ^[୩]

୨୦୦୭ ମସିହାରେ ଆପାଲୁଟାମାଇଡ୍ ବର୍ଣ୍ଣନା କରାଯାଇଥିଲା । ^[୬] ଏହା ୨୦୧୮ରେ ଯୁକ୍ତରାଷ୍ଟ୍ର ଏବଂ ୨୦୧୯ରେ ୟୁରୋପରେ ଚିକିତ୍ସା ବ୍ୟବହାର ପାଇଁ ଅନୁମୋଦିତ ହୋଇଥିଲା। ^[୨] ^[୭] ^[୩] ଯୁକ୍ତରାଜ୍ୟରେ ୨୦୨୧ ସୁଦ୍ଧା ଔଷଧର ମୂଲ୍ୟ ପ୍ରାୟ ୨୭୦୦ ପାଉଣ୍ଡ ଥିଲା । ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଏହି ପରିମାଣର ମୂଲ୍ୟ ପ୍ରାୟ ୧୨,୫୦୦ । ^[୮]

ଆଧାର

↑ ^୧.୦ ^୧.୧ "Apalutamide (Erleada) Use During Pregnancy". Drugs.com. 20 July 2020. Archived from the original on 29 November 2020. Retrieved 28 September 2020.
↑ ^୨.୦୦ ^୨.୦୧ ^୨.୦୨ ^୨.୦୩ ^୨.୦୪ ^୨.୦୫ ^୨.୦୬ ^୨.୦୭ ^୨.୦୮ ^୨.୦୯ ^୨.୧୦ ^୨.୧୧ ^୨.୧୨ ^୨.୧୩ ^୨.୧୪ ^୨.୧୫ ^୨.୧୬ "Erleada- apalutamide tablet, film coated". DailyMed. 27 October 2020. Archived from the original on 9 November 2020. Retrieved 8 November 2020.
↑ ^୩.୦ ^୩.୧ ^୩.୨ ^୩.୩ "Erleada". Archived from the original on 28 December 2020. Retrieved 14 January 2022.
↑ Rathkopf DE, Morris MJ, Fox JJ, Danila DC, Slovin SF, Hager JH, et al. (October 2013). "Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer". Journal of Clinical Oncology. 31 (28): 3525–30. doi:10.1200/JCO.2013.50.1684. PMC 3782148. PMID 24002508.
↑ "Apalutamide Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Retrieved 14 January 2022.
↑ "Espacenet - Original document". Archived from the original on 4 November 2021. Retrieved 25 August 2021.
↑ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 990. ISBN 978-0857114105.
↑ "Erleada Prices, Coupons & Patient Assistance Programs". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 15 January 2021. Retrieved 14 January 2022.

[Drugs.com_pregnancy-1] ୧.୦ ^୧.୧ "Apalutamide (Erleada) Use During Pregnancy". Drugs.com. 20 July 2020. Archived from the original on 29 November 2020. Retrieved 28 September 2020.

[PI2022-2] ୨.୦୦ ^୨.୦୧ ^୨.୦୨ ^୨.୦୩ ^୨.୦୪ ^୨.୦୫ ^୨.୦୬ ^୨.୦୭ ^୨.୦୮ ^୨.୦୯ ^୨.୧୦ ^୨.୧୧ ^୨.୧୨ ^୨.୧୩ ^୨.୧୪ ^୨.୧୫ ^୨.୧୬ "Erleada- apalutamide tablet, film coated". DailyMed. 27 October 2020. Archived from the original on 9 November 2020. Retrieved 8 November 2020.

[EPAR2022-3] ୩.୦ ^୩.୧ ^୩.୨ ^୩.୩ "Erleada". Archived from the original on 28 December 2020. Retrieved 14 January 2022.

[RathkopfMorris2013-4] Rathkopf DE, Morris MJ, Fox JJ, Danila DC, Slovin SF, Hager JH, et al. (October 2013). "Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer". Journal of Clinical Oncology. 31 (28): 3525–30. doi:10.1200/JCO.2013.50.1684. PMC 3782148. PMID 24002508.

[AHFS2022-5] "Apalutamide Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Retrieved 14 January 2022.

[Patent2007-6] "Espacenet - Original document". Archived from the original on 4 November 2021. Retrieved 25 August 2021.

[BNF81-7] BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 990. ISBN 978-0857114105.

[8] "Erleada Prices, Coupons & Patient Assistance Programs". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 15 January 2021. Retrieved 14 January 2022.

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