କୋବିମେଟିନିବ

କୋବିମେଟିନିବ
Clinical data
Pronunciation	/ˌkoʊbɪˈmɛtɪnɪb/ KOH-bim-ET-i-nib
Trade names	Cotellic
Synonyms	GDC-0973, XL-518
AHFS/Drugs.com	monograph
MedlinePlus	a615057
data	EU EMA: yes; US DailyMed: Cobimetinib;
Pregnancy; category	AU: D ; ;
Routes of; administration	By mouth (tablets)
Legal status
Legal status	AU: S4 (Prescription only) ; CA: ℞-only ; UK: POM (Prescription only) ; US: ℞-only ; EU: Rx-only ; ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	reported from 28% to 46%
Protein binding	95%
Metabolism	Intestinal and low liver clearance (mostly CYP3A4 oxidation and UGT2B7 glucuronidation)
Elimination half-life	44 hours (mean)
Excretion	Feces (76–77%), urine (17.9–18%) (after oral and IV administration)
Identifiers
	IUPAC name (S)-[3,4-Difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl] methanone;
Chemical and physical data
Formula	C21H21F3IN3O2
Molar mass	୫୩୧.୩୨ g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O;
	InChI InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m0/s1; Key:BSMCAPRUBJMWDF-KRWDZBQOSA-N;

କୋବିମେଟିନିବ (ଇଂରାଜୀ ଭାଷାରେ Cobimetinib), ଅନ୍ୟମାନଙ୍କ ମଧ୍ୟରେ କୋଟେଲିକ ବେପାର ନାମରେ ବିକ୍ରି ହେଉଛି, ଏକ ଔଷଧ ଯାହା ମେଲାନୋମା ରୋଗର ଚିକିତ୍ସା ପାଇଁ ବ୍ୟବହୃତ ହୁଏ ।^[୧] ନିର୍ଦ୍ଦିଷ୍ଟ ଭାବରେ ଏହା ବିଆରଏଏଫ ଭି୬୦୦କେ (BRAF V600E) କିମ୍ବା ଭି୬୦୦କେ (V600K) ମ୍ୟୁଟେସନ୍ ସହିତ ଆଗେଇ ଯାଇଥିବା ରୋଗ ପାଇଁ ବ୍ୟବହୃତ ହୁଏ ।^[୧] ଏହା ଭେମୁରାଫେନିବ ସହିତ ଏକତ୍ର ବ୍ୟବହୃତ ହୁଏ ।^[୧] ଯୁକ୍ତରାଜ୍ୟରେ ଏହାର ବ୍ୟବହାରକୁ ସୁପାରିଶ କରାଯାଏ ନାହିଁ ।^[୫] ଏହା ପାଟିରେ ଦିଆଯାଏ ।^[୧]

ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ତରଳ ଝାଡ଼ା, ରାସ, ଅଇ, ଜ୍ୱର, ଆତପଦାହ, ଯକୃତ ସମସ୍ୟା କିମ୍ବା ମାଂସପେଶୀ ନଷ୍ଟ ହୋଇପାରେ ।^[୨] ଅନ୍ୟ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ରକ୍ତସ୍ରାବ, କାର୍ଡ଼ିଓମାୟୋପାଥି ଏବଂ ରେଟିନା ଶିରା ଅବରୋଧ ହୋଇପାରେ ।^[୧] ଗର୍ଭାବସ୍ଥାରେ ବ୍ୟବହାର କଲେ ଶିଶୁର କ୍ଷତି ହୋଇପାରେ ।^[୧] ଏହା ଏକ ଏମଇକେ (MEK) ପ୍ରତିରୋଧକ ।^[୧]

୨୦୧୫ ମସିହାରେ ଆମେରିକା ଏବଂ ୟୁରୋପରେ ଡାକ୍ତରୀ ବ୍ୟବହାର ପାଇଁ କୋବିମେଟିନିବ ଅନୁମୋଦିତ ହୋଇଥିଲା ।^[୧] ^[୨] ଯୁକ୍ତରାଜ୍ୟରେ ୪ ସପ୍ତାହର ଚିକିତ୍ସା ପାଇଁ ୨୦୨୧ ସୁଦ୍ଧା ୪୨୭୫ ପାଉଣ୍ଡ ଖର୍ଚ୍ଚ ହେଉଥିଲା ।^[୫] ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଏହି ପରିମାଣର ମୂଲ୍ୟ ପ୍ରାୟ ୭୩୦୦ ଡଲାର ଅଟେ ।^[୬]

ଆଧାର

↑ ^୧.୦୦ ^୧.୦୧ ^୧.୦୨ ^୧.୦୩ ^୧.୦୪ ^୧.୦୫ ^୧.୦୬ ^୧.୦୭ ^୧.୦୮ ^୧.୦୯ ^୧.୧୦ ^୧.୧୧ ^୧.୧୨ ^୧.୧୩ ^୧.୧୪ "Cotellic- cobimetinib tablet, film coated". DailyMed. 5 November 2019. Archived from the original on 4 August 2020. Retrieved 19 October 2020.
↑ ^୨.୦ ^୨.୧ ^୨.୨ "Cotellic". Archived from the original on 20 January 2021. Retrieved 6 January 2022.
↑ ^୩.୦ ^୩.୧ Takahashi RH, Choo EF, Ma S, Wong S, Halladay J, Deng Y, et al. (January 2016). "Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans". Drug Metabolism and Disposition. 44 (1): 28–39. doi:10.1124/dmd.115.066282. PMID 26451002.
↑ Choo E, Takahashi R, Rooney I, Gates M, Deng A, Musib L (January 30, 2014). "Abstract B160: Assessing Human Absorption, Metabolism, Routes of Excretion and the Contribution of Intestinal Metabolism to the Oral Clearance of Cobimetinib, a MEK Inhibitor". Molecular Cancer Therapeutics. 12 (11 Supplement): B160. doi:10.1158/1535-7163.TARG-13-B160.
↑ ^୫.୦ ^୫.୧ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1019. ISBN 978-0857114105.
↑ "Cotellic Prices, Coupons & Patient Assistance Programs". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 26 January 2021. Retrieved 6 January 2022.

[PI2022-1] ୧.୦୦ ^୧.୦୧ ^୧.୦୨ ^୧.୦୩ ^୧.୦୪ ^୧.୦୫ ^୧.୦୬ ^୧.୦୭ ^୧.୦୮ ^୧.୦୯ ^୧.୧୦ ^୧.୧୧ ^୧.୧୨ ^୧.୧୩ ^୧.୧୪ "Cotellic- cobimetinib tablet, film coated". DailyMed. 5 November 2019. Archived from the original on 4 August 2020. Retrieved 19 October 2020.

[EPAR2022-2] ୨.୦ ^୨.୧ ^୨.୨ "Cotellic". Archived from the original on 20 January 2021. Retrieved 6 January 2022.

[Takahashi-3] ୩.୦ ^୩.୧ Takahashi RH, Choo EF, Ma S, Wong S, Halladay J, Deng Y, et al. (January 2016). "Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans". Drug Metabolism and Disposition. 44 (1): 28–39. doi:10.1124/dmd.115.066282. PMID 26451002.

[Choo-4] Choo E, Takahashi R, Rooney I, Gates M, Deng A, Musib L (January 30, 2014). "Abstract B160: Assessing Human Absorption, Metabolism, Routes of Excretion and the Contribution of Intestinal Metabolism to the Oral Clearance of Cobimetinib, a MEK Inhibitor". Molecular Cancer Therapeutics. 12 (11 Supplement): B160. doi:10.1158/1535-7163.TARG-13-B160.

[BNF81-5] ୫.୦ ^୫.୧ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1019. ISBN 978-0857114105.

[6] "Cotellic Prices, Coupons & Patient Assistance Programs". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 26 January 2021. Retrieved 6 January 2022.

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[୫]

[୨]

[୩]

[୪]

[୬]

Clinical data

Pronunciation	/ˌkoʊbɪˈmɛtɪnɪb/ KOH-bim-ET-i-nib
Trade names	Cotellic
Synonyms	GDC-0973, XL-518
AHFS/Drugs.com	monograph
MedlinePlus	a615057
data	EU EMA: yes US DailyMed: Cobimetinib
Pregnancy category	AU: D
Routes of administration	By mouth (tablets)^[୧]
Legal status
Legal status	AU: S4 (Prescription only) CA: ℞-only UK: POM (Prescription only) US: ℞-only ^[୧] EU: Rx-only ^[୨] ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	reported from 28%^[୩] to 46%^[୧]
Protein binding	95%^[୧]
Metabolism	Intestinal and low liver clearance (mostly CYP3A4 oxidation and UGT2B7 glucuronidation)^[୧]^[୩]
Elimination half-life	44 hours (mean)^[୧]
Excretion	Feces (76–77%), urine (17.9–18%) (after oral and IV administration)^[୧]^[୪]
Identifiers
IUPAC name (S)-[3,4-Difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl] methanone
Chemical and physical data
Formula	C₂₁H₂₁F₃IN₃O₂
Molar mass	୫୩୧.୩୨ g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O
InChI InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m0/s1 Key:BSMCAPRUBJMWDF-KRWDZBQOSA-N