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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5979_Библиотеки_им_академика_М_И_Перельмана
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6
Table 1.1 (continued)
Drug name Target kinase
Protein substrate
Phosphorylation site
Binding
mode Medical use
PDB Code and
Refs.
Selpercatinib RET Tyrosine Type I NSCLC/thyroid cancer 7JU6 [63]
Selumetinib MAPK/MEK Serine/Threonine Type III Neurobromatosis type 1 4U7Z [66]
Sorafenib VEGFR/FLT3/KIT Tyrosine Type II RCC, HCC, thyroid cancer 4ASD [23]
Sunitinib PDGFR/FLT3/KIT Tyrosine Type I Renal cancer 3G0E [67]
Tepotinib c-MET Tyrosine Type I NSCLC 4R1V [68]
Tofacitinib JAK Tyrosine Type I Rheumatoid arthritis 3LXK [69]
Trametinib MEK Serine/Threonine Type III Melanoma 7JUR [70]
Trilaciclib CDK4/6 Serine/Threonine NR Bone marrow suppression NR
Tucatinib HER2 Tyrosine NR Breast cancer NR
Umbralisib PI3K Inositol/Serine/
Threonine
Type I Marginal zone lymphoma (MZL), follicular
lymphoma
NR
Upadacitinib JAK Tyrosine NR Rheumatoid arthritis NR
Vandetanib VEGFR/EGFR/RET Tyrosine Type I Thyroid cancer 2IVU [71]
Vemurafenib BRAF Serine/Threonine Type I Melanoma 3OG7 [72]
Volasertib PLK1 Serine/Threonine Type I AML 3FC2 [73]
Zanubrutinib BTK Tyrosine Covalent MCL 6J6M [74]
NR not reported
1 An Overview ofProtein Kinase Inhibitors
https://t.me/med1917
7
Table 1.2 FDA-approved kinase inhibitors’ name, structure, MW, and company information
Year Drug structure and generic name (trade name) MW Company
1999
OO
HO
O
O
N
O
OO OH
O
O
O
HO
Rapamycin (Rapamune, Sirolimus)
914 Wyeth
2001
N
NN
H
N
NH
O
N
N
Imatinib (Gleevec)
494 Novartis
2003
Cl
F
HN
N
N
ON
O
O
Getinib (Iressa)
447 Astra
Zeneca
2004
HN
N
NO
O
O
O
Erlotinib (Tarceva)
393 Genentech
2005
CF
3
Cl
N
H
N
H
O
O
N
O
N
H
Sorafenib (Nexavar)
465 Onyx
(continued)
1.1 Introduction
https://t.me/med1917
8
Table 1.2 (continued)
Year Drug structure and generic name (trade name) MW Company
2006
F
N
H
O
N
H
O
N
H
N
Sunitinib (Sutent)
398 Pzer
2006
Cl
H
N
O
S
N
H
N
NN
M
N
HO
Dasatinib(Sprycel)
488 Bristol Myers Squibb
(BMS)
2007
OO
HO
O
O
N
O
OO OH
O
O
O
O
O
OH
HO
Temsirolimus (Torisel)
1024 Wyeth
2007
N
NN
H
N
ON
H
CF
3
N
N
Nilotinib (Tasigna)
530 Novartis
(continued)
1 An Overview ofProtein Kinase Inhibitors
https://t.me/med1917
9
Table 1.2 (continued)
Year Drug structure and generic name (trade name) MW Company
2007
O
HN
N
N
Cl
F
O
H
N
S
O
O
Lapatinib (Tykerb)
581 GSK
2009
OO
HO
O
O
N
O
OO OH
O
O
O
O
HO
Everolimus (Anitor)
958 Novartis
2009
N
N
N
N
N
H
N
S
O
O
H
2
N
Pazopanib (Votrient)
437 GSK
2011
N
N
H
Cl
O
F
F
NH
S
O
O
Vemurafenib (Zelboraf)
489 Genentech
2011
NNH
2
O
Cl
Cl
F
N
N
HN
Crizotinib (Xalkori)
450 Pzer
(continued)
1.1 Introduction
https://t.me/med1917
10
Table 1.2 (continued)
Year Drug structure and generic name (trade name) MW Company
2011
N
N
N
H
N
N
CN
Ruxolitinib (Jaka)
306 Incyte
2011
N
N
HN
FB
r
O
N
O
Vandetanib (Caprelsa)
475 Astra
Zeneca
2012
N
H
N
N
S
OH
2
N
Axitinib (Inlyta)
386 Pzer
2012
O
Cl
HN
Cl
N
CN
ON
N
O
Bosutinib (Bosul)
530 Wyeth
2012
N
O
MeO
Me
O
H
N
OO
H
N
F
Cabozantinib (Cometriq)
501 Exelixis
2012
N
N
N
O
N
H
F
3
C
N
N
Ponatinib (Iclusig)
533 Ariad
(continued)
1 An Overview ofProtein Kinase Inhibitors
https://t.me/med1917
11
Table 1.2 (continued)
Year Drug structure and generic name (trade name) MW Company
2012
N
O
F
N
H
O
N
H
CF
3
Cl
O
N
H
Rigorafenib (Stivarga)
483 Bayer
2012
N
N
N
H
N
N
O
N
Tofacitinib (Xeljanz)
312 Pzer
2013
N
N
NH
2
S
N
F
H
N
S
O
O
F
F
Dabrafenib (Tanlar)
520 GlaxoSmithKline
(GSK)
2013
NN
N
N
N
O
H
2
N
O
Ibrutinib (Imbruvica)
441 Pharmacyclics/Johnson &
Johnson
2013
HN
N
NO
HN
O
O
Me
2
N
Cl
F
Afatinib (Gilotrif)
486 Boeh-ringer Ingelheim
(BI)
2013
N
N
N
OO
O
N
H
F
I
N
H
O
Trametinib (Mekinist)
615 GSK
(continued)
1.1 Introduction
https://t.me/med1917
12
Table 1.2 (continued)
Year Drug structure and generic name (trade name) MW Company
2014
N
N
OF
HN
N
N
N
HN
Idelalisib (Zydelig)
415 Gilead
2014
NH
O
H
N
N
O
N
N
Nintedanib (Ofev/Vargatef)
540 B.I.
2015
O
H
N
CN
N
N
O
Alectinib (Alecensa)
483 Hoffman
LaRoche
2015
F
F
H
N
F
I
O
N
OH
N
H
Cobimetinib (Cotellic)
531 Genentech
2015
N
O
MeO
O
H
2
N
H
N
H
N
O
Cl
Lenvatinib (Lenvima)
427 Eisai
2015
N
N
N
H
N
HN
NMe
2
O
N
OMe
Osimertinib (Tagrisso)
500 Astra
Zeneca
(continued)
1 An Overview ofProtein Kinase Inhibitors
https://t.me/med1917
13
Table 1.2 (continued)
Year Drug structure and generic name (trade name) MW Company
2015
N
NNO
O
H
N
N
N
HN
Palbociclib (Ibrance)
447 Park Davis
2017
N
N
F
N
N
F
N
H
N
N
N
Abemaciclib (Verzenio)
507 Eli Lilly
2017
N
N
N
NH
2
O
N
H
N
N
O
Acalabrutinib (Calquence)
466 Acerta Pharm
2017
N
N
H
N
HN
P
O
O
N
N
N
Cl
Brigatinib (Alunbrig)
584 Ariad
2017
N
N
N
N
H
O
O
O
N
N
NH
2
N
O
Copanlisib (Aliqopa)
480 Bayer
(continued)
1.1 Introduction
https://t.me/med1917
14
Table 1.2 (continued)
Year Drug structure and generic name (trade name) MW Company
2017
N
H
N
N
O
O
MeO
N
O
Midostaurin (Rydapt)
570 Novartis
2017
HN
NO
HN
O
Me
2
N
Cl
O
CN
N
Neratinib (Nerlynix)
557 Puma
2017
N
N
N
O
NMe
2
H
N
N
N
HN
Ribociclib (Kisqali)
435 Novartis
2018
N
N
F
HN
F
Br
O
H
N
O
HO
Binimetinib (Mektovi)
441 Array
2018
N
N
N
H
N
N
N
CN
S
O
O
Baricitinib (Olumiant)
371 Eli Lilly
(continued)
1 An Overview ofProtein Kinase Inhibitors
https://t.me/med1917
15
Table 1.2 (continued)
Year Drug structure and generic name (trade name) MW Company
2018
HN
N
NMeO
HN
O
N
Cl
F
Dacomitinib (Visimpro)
470 Pzer
2018
N
OCl
HN
N
N
N
HN
Duvelisib (Copiktra)
416 Verastem
2018
N
N
H
N
N
H
O
O
N
N
F
Cl N
H
S
O
O
Encorafenib (Braftovi)
540 Array
2018
N
N
F
N
H
N
H
NN
O
OMe
MeO
Me
O
O
O
P
O
HO
OH
Fostamatinib (Tavalisse)
580 Rigel
2018
N
N
N
H
N
O
O
NH
2
OMe
N
N
N
Giltertinib (Xospata)
553 Astellas
(continued)
1.1 Introduction
https://t.me/med1917
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