Peringatan Keamanan

Neither fostamatinib or R406 were found to be carcinogenic or mutagenic FDA Label. Fostamatinib can cause embryo-fetal mortality or developmental abnormalities at exposures of 0.3-10 times the maximum recommended human dose.

Serious adverse effects include hypertension, neutropenia, diarrhea, and hepatotoxicity FDA Label

Fostamatinib

DB12010

small molecule approved investigational

Deskripsi

Fostamatinib has been investigated for the treatment and basic science of Rheumatoid Arthritis and Immune Thrombocytopenic Purpura (ITP). It was approved on April 17, 2018, under the trade name Tavalisse for use in ITP L2644, FDA Label. Fostamatinib has also been granted orphan drug status by the FDA L2644.

Recently, fostamatinib has been identified as a potential therapeutic for controlling acute respiratory distress syndrome (ARDS) in patients with severe COVID-19 through its ability to modulate the SYK kinase.A235008, A235013, A235018

Struktur Molekul 2D

Berat 580.4595
Wujud -

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) R406 has a half-life of elimination of approximately 15 h [A32934,FDA Label].
Volume Distribusi R406 has an apparent oral volume of distribution of approximately 400 L [A32934].
Klirens (Clearance) R406 has an apparent oral clearance of approximately 300 mL/min [A32934].

Absorpsi

Fostmatinib is the methylene phosphate prodrug of R406, the active metabolite FDA Label. It is extensively hydrolyzed by intestinal alkaline phosphatase. Only negligible amounts of fostamatinib enter systemic circulation A32934,FDA Label. R406 has an absolute bioavailability of 55% and reaches peak plasma concentrations in approximately 1.5 h A32934,FDA Label. Administration with a high calorie, high fat meal increases exposure by 23% and the maximum plasma concentration by 15%. This may lengthen time to peak plasma concentration to approximately 3 h A32934. Exposure to R406 is known to be dose proportional up to 200 mg twice daily FDA Label. R406 accumulates 2-3 fold with twice daily dosing at 100-160 mg.

Metabolisme

Fostamatinib is metabolized in the gut by alkaline phosphatase to the active metabolite R406 FDA Label. R406 is further oxidized by CYP3A4 and glucuronidated by UGT1A9. Plasma metabolites found include an O-glucuronide conjugate, an N-glucuronide conjugate, an O-desmethyl metabolite, and a sulfate conjugate FDA Label,A32936. A 3,5 benzene diol metabolite forms in the feces via processing of the O-desmethyl metabolite by gut bacteria A32936.

Rute Eliminasi

About 80% of R406 is excreted in the feces, primarily as the O-glucuronide conjugate and the O-desmethyl metabolite produced by gut bacteria FDA Label. The remaining 20% is excreted in the urine as the N-glucuronide conjugate.

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of fostamatinib.
  • 2. Take with or without food.

Interaksi Obat

692 Data
Eliglustat The metabolism of Eliglustat can be decreased when combined with Fostamatinib.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Fostamatinib.
Alprostadil The risk or severity of hypotension and priapism can be increased when Fostamatinib is combined with Alprostadil.
Amyl Nitrite The risk or severity of hypotension can be increased when Fostamatinib is combined with Amyl Nitrite.
Dapoxetine The risk or severity of orthostatic hypotension can be increased when Dapoxetine is combined with Fostamatinib.
Riociguat Fostamatinib may increase the hypotensive activities of Riociguat.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Fostamatinib.
Colchicine The metabolism of Colchicine can be decreased when combined with Fostamatinib.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Fostamatinib.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Fostamatinib.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Fostamatinib.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Fostamatinib.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Fostamatinib.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Fostamatinib.
Irinotecan The risk or severity of neutropenia can be increased when Fostamatinib is combined with Irinotecan.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Fostamatinib.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Fostamatinib.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Fostamatinib.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Fostamatinib.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Fostamatinib.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Fostamatinib.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Fostamatinib.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Fostamatinib.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Fostamatinib.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Fostamatinib.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Fostamatinib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Fostamatinib.
Sapropterin Sapropterin may increase the hypotensive activities of Fostamatinib.
Ethanol Ethanol may increase the hypotensive activities of Fostamatinib.
Valsartan Fostamatinib may increase the antihypertensive activities of Valsartan.
Ramipril Fostamatinib may increase the antihypertensive activities of Ramipril.
Esmolol Fostamatinib may increase the antihypertensive activities of Esmolol.
Betaxolol Fostamatinib may increase the antihypertensive activities of Betaxolol.
Reserpine Fostamatinib may increase the antihypertensive activities of Reserpine.
Remikiren Fostamatinib may increase the antihypertensive activities of Remikiren.
Torasemide Fostamatinib may increase the antihypertensive activities of Torasemide.
Bethanidine Fostamatinib may increase the antihypertensive activities of Bethanidine.
Guanadrel Fostamatinib may increase the antihypertensive activities of Guanadrel.
Olmesartan Fostamatinib may increase the antihypertensive activities of Olmesartan.
Chlorthalidone Fostamatinib may increase the antihypertensive activities of Chlorthalidone.
Nitroprusside Fostamatinib may increase the antihypertensive activities of Nitroprusside.
Atenolol Fostamatinib may increase the antihypertensive activities of Atenolol.
Timolol Fostamatinib may increase the antihypertensive activities of Timolol.
Treprostinil Fostamatinib may increase the antihypertensive activities of Treprostinil.
Amlodipine Fostamatinib may increase the antihypertensive activities of Amlodipine.
Nimodipine Fostamatinib may increase the antihypertensive activities of Nimodipine.
Bendroflumethiazide Fostamatinib may increase the antihypertensive activities of Bendroflumethiazide.
Fosinopril Fostamatinib may increase the antihypertensive activities of Fosinopril.
Trandolapril Fostamatinib may increase the antihypertensive activities of Trandolapril.
Metolazone Fostamatinib may increase the antihypertensive activities of Metolazone.
Lercanidipine Fostamatinib may increase the antihypertensive activities of Lercanidipine.
Benazepril Fostamatinib may increase the antihypertensive activities of Benazepril.
Bosentan Fostamatinib may increase the antihypertensive activities of Bosentan.
Propranolol Fostamatinib may increase the antihypertensive activities of Propranolol.
Enalapril Fostamatinib may increase the antihypertensive activities of Enalapril.
Cyclothiazide Fostamatinib may increase the antihypertensive activities of Cyclothiazide.
Bisoprolol Fostamatinib may increase the antihypertensive activities of Bisoprolol.
Candoxatril Fostamatinib may increase the antihypertensive activities of Candoxatril.
Guanabenz Fostamatinib may increase the antihypertensive activities of Guanabenz.
Mecamylamine Fostamatinib may increase the antihypertensive activities of Mecamylamine.
Moexipril Fostamatinib may increase the antihypertensive activities of Moexipril.
Lisinopril Fostamatinib may increase the antihypertensive activities of Lisinopril.
Metyrosine Fostamatinib may increase the antihypertensive activities of Metyrosine.
Hydroflumethiazide Fostamatinib may increase the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Fostamatinib may increase the antihypertensive activities of Cryptenamine.
Perindopril Fostamatinib may increase the antihypertensive activities of Perindopril.
Candesartan cilexetil Fostamatinib may increase the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Fostamatinib may increase the antihypertensive activities of Fenoldopam.
Indapamide Fostamatinib may increase the antihypertensive activities of Indapamide.
Alprenolol Fostamatinib may increase the antihypertensive activities of Alprenolol.
Eprosartan Fostamatinib may increase the antihypertensive activities of Eprosartan.
Chlorothiazide Fostamatinib may increase the antihypertensive activities of Chlorothiazide.
Quinapril Fostamatinib may increase the antihypertensive activities of Quinapril.
Omapatrilat Fostamatinib may increase the antihypertensive activities of Omapatrilat.
Pindolol Fostamatinib may increase the antihypertensive activities of Pindolol.
Telmisartan Fostamatinib may increase the antihypertensive activities of Telmisartan.
Methyldopa Fostamatinib may increase the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Fostamatinib may increase the antihypertensive activities of Hydrochlorothiazide.
Guanfacine Fostamatinib may increase the antihypertensive activities of Guanfacine.
Trichlormethiazide Fostamatinib may increase the antihypertensive activities of Trichlormethiazide.
Irbesartan Fostamatinib may increase the antihypertensive activities of Irbesartan.
Nitrendipine Fostamatinib may increase the antihypertensive activities of Nitrendipine.
Deserpidine Fostamatinib may increase the antihypertensive activities of Deserpidine.
Pentolinium Fostamatinib may increase the antihypertensive activities of Pentolinium.
Trimethaphan Fostamatinib may increase the antihypertensive activities of Trimethaphan.
Diazoxide Fostamatinib may increase the antihypertensive activities of Diazoxide.
Bretylium Fostamatinib may increase the antihypertensive activities of Bretylium.
Guanethidine Fostamatinib may increase the antihypertensive activities of Guanethidine.
Rescinnamine Fostamatinib may increase the antihypertensive activities of Rescinnamine.
Acebutolol Fostamatinib may increase the antihypertensive activities of Acebutolol.
Captopril Fostamatinib may increase the antihypertensive activities of Captopril.
Nadolol Fostamatinib may increase the antihypertensive activities of Nadolol.
Epoprostenol Fostamatinib may increase the antihypertensive activities of Epoprostenol.
Bepridil Fostamatinib may increase the antihypertensive activities of Bepridil.
Hydralazine Fostamatinib may increase the antihypertensive activities of Hydralazine.
Practolol Fostamatinib may increase the antihypertensive activities of Practolol.
Polythiazide Fostamatinib may increase the antihypertensive activities of Polythiazide.
Cilazapril Fostamatinib may increase the antihypertensive activities of Cilazapril.
Saprisartan Fostamatinib may increase the antihypertensive activities of Saprisartan.
Spirapril Fostamatinib may increase the antihypertensive activities of Spirapril.

Target Protein

Tyrosine-protein kinase SYK SYK
Adenosine receptor A3 ADORA3
Synaptic vesicular amine transporter SLC18A2
Fatty-acid amide hydrolase 1 FAAH
Equilibrative nucleoside transporter 1 SLC29A1
UDP-glucuronosyltransferase 1A1 UGT1A1
cGMP-specific 3',5'-cyclic phosphodiesterase PDE5A
Polyunsaturated fatty acid 5-lipoxygenase ALOX5
Cathepsin S CTSS
Procathepsin L CTSL
Tyrosine-protein kinase ABL1 ABL1
Calcium-dependent protein kinase 1 CPK1
Serine/threonine-protein kinase PknB pknB
Ribosomal protein S6 kinase alpha-6 RPS6KA6
Non-receptor tyrosine-protein kinase TYK2 TYK2
Atypical kinase COQ8A, mitochondrial COQ8A
Tyrosine-protein kinase JAK1 JAK1
Hepatocyte growth factor receptor MET
Serine/threonine-protein kinase NIM1 NIM1K
Serine/threonine-protein kinase 26 STK26
cAMP-dependent protein kinase catalytic subunit alpha PRKACA
Serine/threonine-protein kinase 24 STK24
Serine/threonine-protein kinase 3 STK3
Tyrosine-protein kinase Tec TEC
Serine/threonine-protein kinase 33 STK33
Serine/threonine-protein kinase 35 STK35
Serine/threonine-protein kinase 36 STK36
Serine/threonine-protein kinase 38 STK38
Serine/threonine-protein kinase 38-like STK38L
STE20/SPS1-related proline-alanine-rich protein kinase STK39
Serine/threonine-protein kinase TAO1 TAOK1
Serine/threonine-protein kinase TAO2 TAOK2
Serine/threonine-protein kinase TAO3 TAOK3
Serine/threonine-protein kinase TBK1 TBK1
Angiopoietin-1 receptor TEK
Dual specificity testis-specific protein kinase 1 TESK1
TGF-beta receptor type-1 TGFBR1
TGF-beta receptor type-2 TGFBR2
Tyrosine-protein kinase receptor Tie-1 TIE1
Serine/threonine-protein kinase tousled-like 1 TLK1
Serine/threonine-protein kinase tousled-like 2 TLK2
TRAF2 and NCK-interacting protein kinase TNIK
Non-receptor tyrosine-protein kinase TNK1 TNK1
Activated CDC42 kinase 1 TNK2
Serine/threonine-protein kinase TNNI3K TNNI3K
Testis-specific serine/threonine-protein kinase 1 TSSK1B
Dual specificity protein kinase TTK TTK
Tyrosine-protein kinase TXK TXK
Tyrosine-protein kinase receptor TYRO3 TYRO3
Serine/threonine-protein kinase ULK1 ULK1
Serine/threonine-protein kinase ULK2 ULK2
Serine/threonine-protein kinase ULK3 ULK3
Wee1-like protein kinase WEE1
Tyrosine-protein kinase Yes YES1
Mitogen-activated protein kinase kinase kinase 19 MAP3K19
Mitogen-activated protein kinase kinase kinase 20 MAP3K20
Tyrosine-protein kinase ZAP-70 ZAP70
AP2-associated protein kinase 1 AAK1
Tyrosine-protein kinase ABL2 ABL2
Activin receptor type-1 ACVR1
Activin receptor type-1B ACVR1B
Atypical kinase COQ8B, mitochondrial COQ8B
ALK tyrosine kinase receptor ALK
Ankyrin repeat and protein kinase domain-containing protein 1 ANKK1
Aurora kinase A AURKA
Aurora kinase B AURKB
Aurora kinase C AURKC
Tyrosine-protein kinase receptor UFO AXL
Tyrosine-protein kinase Blk BLK
BMP-2-inducible protein kinase BMP2K
Bone morphogenetic protein receptor type-1B BMPR1B
Bone morphogenetic protein receptor type-2 BMPR2
Cytoplasmic tyrosine-protein kinase BMX BMX
Serine/threonine-protein kinase B-raf BRAF
Tyrosine-protein kinase BTK BTK
Calcium/calmodulin-dependent protein kinase type 1 CAMK1
Calcium/calmodulin-dependent protein kinase type 1D CAMK1D
Calcium/calmodulin-dependent protein kinase type 1G CAMK1G
Calcium/calmodulin-dependent protein kinase type II subunit alpha CAMK2A
Calcium/calmodulin-dependent protein kinase type II subunit beta CAMK2B
Calcium/calmodulin-dependent protein kinase type II subunit delta CAMK2D
Calcium/calmodulin-dependent protein kinase type II subunit gamma CAMK2G
Calcium/calmodulin-dependent protein kinase kinase 1 CAMKK1
Calcium/calmodulin-dependent protein kinase kinase 2 CAMKK2
Peripheral plasma membrane protein CASK CASK
Kappa-casein CSN3
Cyclin-dependent kinase 1 CDK1
Serine/threonine-protein kinase MRCK gamma CDC42BPG
Cyclin-dependent kinase 4 CDK4
Cyclin-dependent kinase-like 1 CDKL1
Cyclin-dependent kinase-like 2 CDKL2
Serine/threonine-protein kinase Chk1 CHEK1
Serine/threonine-protein kinase Chk2 CHEK2
Citron Rho-interacting kinase CIT
Dual specificity protein kinase CLK1 CLK1
Dual specificity protein kinase CLK2 CLK2
Dual specificity protein kinase CLK3 CLK3
Dual specificity protein kinase CLK4 CLK4
Macrophage colony-stimulating factor 1 receptor CSF1R
Tyrosine-protein kinase CSK CSK
Casein kinase I isoform alpha CSNK1A1
Casein kinase II subunit alpha CSNK2A1
Casein kinase II subunit alpha' CSNK2A2
Death-associated protein kinase 1 DAPK1
Death-associated protein kinase 2 DAPK2
Death-associated protein kinase 3 DAPK3
Serine/threonine-protein kinase DCLK1 DCLK1
Serine/threonine-protein kinase DCLK2 DCLK2
Serine/threonine-protein kinase DCLK3 DCLK3
Epithelial discoidin domain-containing receptor 1 DDR1
Discoidin domain-containing receptor 2 DDR2
Dual specificity tyrosine-phosphorylation-regulated kinase 1A DYRK1A
Dual specificity tyrosine-phosphorylation-regulated kinase 1B DYRK1B
Epidermal growth factor receptor EGFR
Eukaryotic translation initiation factor 2-alpha kinase 1 EIF2AK1
Interferon-induced, double-stranded RNA-activated protein kinase EIF2AK2
eIF-2-alpha kinase GCN2 EIF2AK4
Ephrin type-A receptor 1 EPHA1
Ephrin type-A receptor 2 EPHA2
Ephrin type-A receptor 3 EPHA3
Ephrin type-A receptor 4 EPHA4
Ephrin type-A receptor 5 EPHA5
Ephrin type-A receptor 6 EPHA6
Ephrin type-A receptor 7 EPHA7
Ephrin type-A receptor 8 EPHA8
Ephrin type-B receptor 1 EPHB1
Ephrin type-B receptor 2 EPHB2
Ephrin type-B receptor 4 EPHB4
Ephrin type-B receptor 6 EPHB6
Receptor tyrosine-protein kinase erbB-2 ERBB2
Receptor tyrosine-protein kinase erbB-4 ERBB4
Serine/threonine-protein kinase/endoribonuclease IRE1 ERN1
Tyrosine-protein kinase Fer FER
Tyrosine-protein kinase Fes/Fps FES
Fibroblast growth factor receptor 1 FGFR1
Fibroblast growth factor receptor 2 FGFR2
Fibroblast growth factor receptor 3 FGFR3
Tyrosine-protein kinase Fgr FGR
Vascular endothelial growth factor receptor 1 FLT1
Receptor-type tyrosine-protein kinase FLT3 FLT3
Vascular endothelial growth factor receptor 3 FLT4
Serine/threonine-protein kinase mTOR MTOR
Tyrosine-protein kinase FRK FRK
Tyrosine-protein kinase Fyn FYN
Cyclin-G-associated kinase GAK
Glycogen synthase kinase-3 alpha GSK3A
Glycogen synthase kinase-3 beta GSK3B
Tyrosine-protein kinase HCK HCK
Homeodomain-interacting protein kinase 2 HIPK2
Homeodomain-interacting protein kinase 3 HIPK3
Serine/threonine-protein kinase ICK CILK1
Inhibitor of nuclear factor kappa-B kinase subunit beta IKBKB
Inhibitor of nuclear factor kappa-B kinase subunit epsilon IKBKE
Insulin receptor INSR
Insulin receptor-related protein INSRR
Interleukin-1 receptor-associated kinase 1 IRAK1
Interleukin-1 receptor-associated kinase 3 IRAK3
Interleukin-1 receptor-associated kinase 4 IRAK4
Tyrosine-protein kinase ITK/TSK ITK
Tyrosine-protein kinase JAK2 JAK2
Tyrosine-protein kinase JAK3 JAK3
Vascular endothelial growth factor receptor 2 KDR
Serine/threonine-protein kinase SIK3 SIK3
Mast/stem cell growth factor receptor Kit KIT
Serine/threonine-protein kinase LATS1 LATS1
Tyrosine-protein kinase Lck LCK
LIM domain kinase 1 LIMK1
LIM domain kinase 2 LIMK2
Leucine-rich repeat serine/threonine-protein kinase 2 LRRK2
Leukocyte tyrosine kinase receptor LTK
Tyrosine-protein kinase Lyn LYN
Dual specificity mitogen-activated protein kinase kinase 2 MAP2K2
Dual specificity mitogen-activated protein kinase kinase 3 MAP2K3
Dual specificity mitogen-activated protein kinase kinase 5 MAP2K5
Dual specificity mitogen-activated protein kinase kinase 6 MAP2K6
Mitogen-activated protein kinase kinase kinase 1 MAP3K1
Mitogen-activated protein kinase kinase kinase 10 MAP3K10
Mitogen-activated protein kinase kinase kinase 11 MAP3K11
Mitogen-activated protein kinase kinase kinase 12 MAP3K12
Mitogen-activated protein kinase kinase kinase 13 MAP3K13
Mitogen-activated protein kinase kinase kinase 15 MAP3K15
Mitogen-activated protein kinase kinase kinase 2 MAP3K2
Mitogen-activated protein kinase kinase kinase 3 MAP3K3
Mitogen-activated protein kinase kinase kinase 4 MAP3K4
Mitogen-activated protein kinase kinase kinase 6 MAP3K6
Mitogen-activated protein kinase kinase kinase 9 MAP3K9
Mitogen-activated protein kinase kinase kinase kinase 1 MAP4K1
Mitogen-activated protein kinase kinase kinase kinase 2 MAP4K2
Mitogen-activated protein kinase kinase kinase kinase 3 MAP4K3
Mitogen-activated protein kinase kinase kinase kinase 4 MAP4K4
Mitogen-activated protein kinase kinase kinase kinase 5 MAP4K5
Mitogen-activated protein kinase 10 MAPK10
Mitogen-activated protein kinase 13 MAPK13
Mitogen-activated protein kinase 14 MAPK14
Mitogen-activated protein kinase 15 MAPK15
Mitogen-activated protein kinase 4 MAPK4
Mitogen-activated protein kinase 7 MAPK7
Mitogen-activated protein kinase 9 MAPK9
MAP kinase-activated protein kinase 5 MAPKAPK5
Serine/threonine-protein kinase MARK1 MARK1
Serine/threonine-protein kinase MARK2 MARK2
MAP/microtubule affinity-regulating kinase 3 MARK3
MAP/microtubule affinity-regulating kinase 4 MARK4
CLIP-associating protein 1 CLASP1
Microtubule-associated serine/threonine-protein kinase 1 MAST1
Megakaryocyte-associated tyrosine-protein kinase MATK
Maternal embryonic leucine zipper kinase MELK
Tyrosine-protein kinase Mer MERTK
Misshapen-like kinase 1 MINK1
MAP kinase-interacting serine/threonine-protein kinase 1 MKNK1
MAP kinase-interacting serine/threonine-protein kinase 2 MKNK2
Macrophage-stimulating protein receptor MST1R
Muscle, skeletal receptor tyrosine-protein kinase MUSK
Myosin light chain kinase, smooth muscle MYLK
Myosin light chain kinase 2, skeletal/cardiac muscle MYLK2
Myosin light chain kinase 3 MYLK3
Myosin light chain kinase family member 4 MYLK4
Myosin-IIIa MYO3A
Serine/threonine-protein kinase Nek1 NEK1
Serine/threonine-protein kinase Nek11 NEK11
Serine/threonine-protein kinase Nek2 NEK2
Serine/threonine-protein kinase Nek3 NEK3
Serine/threonine-protein kinase Nek4 NEK4
Serine/threonine-protein kinase Nek5 NEK5
Serine/threonine-protein kinase Nek9 NEK9
High affinity nerve growth factor receptor NTRK1
BDNF/NT-3 growth factors receptor NTRK2
NT-3 growth factor receptor NTRK3
NUAK family SNF1-like kinase 1 NUAK1
NUAK family SNF1-like kinase 2 NUAK2
Serine/threonine-protein kinase OSR1 OXSR1
Serine/threonine-protein kinase PAK 1 PAK1
Serine/threonine-protein kinase PAK 2 PAK2
Serine/threonine-protein kinase PAK 3 PAK3
Serine/threonine-protein kinase PAK 4 PAK4
Serine/threonine-protein kinase PAK 6 PAK6
Serine/threonine-protein kinase PAK 5 PAK5
Cyclin-dependent kinase 16 CDK16
Cyclin-dependent kinase 17 CDK17
Platelet-derived growth factor receptor alpha PDGFRA
Platelet-derived growth factor receptor beta PDGFRB
3-phosphoinositide-dependent protein kinase 1 PDPK1
Cyclin-dependent kinase 15 CDK15
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform PHKG1
Phosphatidylinositol 4-kinase beta PI4KB
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta PIK3C2B
Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma PIK3C2G
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform PIK3CD
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform PIK3CG
Serine/threonine-protein kinase pim-1 PIM1
Serine/threonine-protein kinase pim-3 PIM3
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta PIP4K2B
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma PIP4K2C
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase PKMYT1
Serine/threonine-protein kinase N1 PKN1
Serine/threonine-protein kinase N2 PKN2
Serine/threonine-protein kinase PLK1 PLK1
Serine/threonine-protein kinase PLK2 PLK2
Serine/threonine-protein kinase PLK3 PLK3
Serine/threonine-protein kinase PLK4 PLK4
5'-AMP-activated protein kinase catalytic subunit alpha-1 PRKAA1
5'-AMP-activated protein kinase PRKAA1
cAMP-dependent protein kinase catalytic subunit beta PRKACB
Protein kinase C delta type PRKCD
Protein kinase C epsilon type PRKCE
Protein kinase C gamma type PRKCG
Protein kinase C iota type PRKCI
Protein kinase C theta type PRKCQ
Serine/threonine-protein kinase D1 PRKD1
cGMP-dependent protein kinase 2 PRKG2
Serine/threonine-protein kinase PRP4 homolog PRP4K
Focal adhesion kinase 1 PTK2
Protein-tyrosine kinase 2-beta PTK2B
Protein-tyrosine kinase 6 PTK6
RAF proto-oncogene serine/threonine-protein kinase RAF1
Proto-oncogene tyrosine-protein kinase receptor Ret RET
Serine/threonine-protein kinase RIO1 RIOK1
Serine/threonine-protein kinase RIO2 RIOK2
Serine/threonine-protein kinase RIO3 RIOK3
Receptor-interacting serine/threonine-protein kinase 1 RIPK1
Receptor-interacting serine/threonine-protein kinase 2 RIPK2
Receptor-interacting serine/threonine-protein kinase 4 RIPK4
Rho-associated protein kinase 2 ROCK2
Proto-oncogene tyrosine-protein kinase ROS ROS1
Ribosomal protein S6 kinase alpha-1 RPS6KA1
Ribosomal protein S6 kinase alpha-3 RPS6KA3
Serine/threonine-protein kinase SBK1 SBK1
Uncharacterized serine/threonine-protein kinase SBK3 SBK3
Serine/threonine-protein kinase Sgk3 SGK3
Serine/threonine-protein kinase SIK1 SIK1
Serine/threonine-protein kinase SIK2 SIK2
STE20-like serine/threonine-protein kinase SLK
SNF-related serine/threonine-protein kinase SNRK
Proto-oncogene tyrosine-protein kinase Src SRC
Tyrosine-protein kinase Srms SRMS
Serine/threonine-protein kinase 10 STK10
Serine/threonine-protein kinase 16 STK16
Serine/threonine-protein kinase 17A STK17A
Serine/threonine-protein kinase 17B STK17B
Serine/threonine-protein kinase 32A STK32A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20553955
    Riccaboni M, Bianchi I, Petrillo P: Spleen tyrosine kinases: biology, therapeutic targets and drugs. Drug Discov Today. 2010 Jul;15(13-14):517-30. doi: 10.1016/j.drudis.2010.05.001. Epub 2010 May 27.
  • PMID: 16946104
    Braselmann S, Taylor V, Zhao H, Wang S, Sylvain C, Baluom M, Qu K, Herlaar E, Lau A, Young C, Wong BR, Lovell S, Sun T, Park G, Argade A, Jurcevic S, Pine P, Singh R, Grossbard EB, Payan DG, Masuda ES: R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. doi: 10.1124/jpet.106.109058. Epub 2006 Aug 31.
  • PMID: 20053395
    Sanderson MP, Gelling SJ, Rippmann JF, Schnapp A: Comparison of the anti-allergic activity of Syk inhibitors with optimized Syk siRNAs in FcepsilonRI-activated RBL-2H3 basophilic cells. Cell Immunol. 2010;262(1):28-34. doi: 10.1016/j.cellimm.2009.12.004. Epub 2009 Dec 14.
  • PMID: 12517949
    Sedlik C, Orbach D, Veron P, Schweighoffer E, Colucci F, Gamberale R, Ioan-Facsinay A, Verbeek S, Ricciardi-Castagnoli P, Bonnerot C, Tybulewicz VL, Di Santo J, Amigorena S: A critical role for Syk protein tyrosine kinase in Fc receptor-mediated antigen presentation and induction of dendritic cell maturation. J Immunol. 2003 Jan 15;170(2):846-52.
  • PMID: 26516587
    Rolf MG, Curwen JO, Veldman-Jones M, Eberlein C, Wang J, Harmer A, Hellawell CJ, Braddock M: In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib. Pharmacol Res Perspect. 2015 Oct;3(5):e00175. doi: 10.1002/prp2.175. Epub 2015 Sep 4.
  • PMID: 23190017
    Baluom M, Grossbard EB, Mant T, Lau DT: Pharmacokinetics of fostamatinib, a spleen tyrosine kinase (SYK) inhibitor, in healthy human subjects following single and multiple oral dosing in three phase I studies. Br J Clin Pharmacol. 2013 Jul;76(1):78-88. doi: 10.1111/bcp.12048.
  • PMID: 20371637
    Sweeny DJ, Li W, Clough J, Bhamidipati S, Singh R, Park G, Baluom M, Grossbard E, Lau DT: Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans: contribution of hepatic and gut bacterial processes to the overall biotransformation. Drug Metab Dispos. 2010 Jul;38(7):1166-76. doi: 10.1124/dmd.110.032151. Epub 2010 Apr 6.
  • PMID: 33367731
    Strich JR, Ramos-Benitez MJ, Randazzo D, Stein SR, Babyak A, Davey RT, Suffredini AF, Childs RW, Chertow DS: Fostamatinib Inhibits Neutrophils Extracellular Traps Induced by COVID-19 Patient Plasma: A Potential Therapeutic. J Infect Dis. 2021 Mar 29;223(6):981-984. doi: 10.1093/infdis/jiaa789.
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Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Tavalisse
    Tablet • 100 mg • Oral • Canada • Approved
  • Tavalisse
    Tablet • 150 mg • Oral • Canada • Approved
  • Tavalisse
    Tablet • 100 mg/1 • Oral • US • Approved
  • Tavalisse
    Tablet • 150 mg/1 • Oral • US • Approved
  • Tavlesse
    Tablet, film coated • 100 mg • Oral • EU • Approved
  • Tavlesse
    Tablet, film coated • 150 mg • Oral • EU • Approved

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