General Information of Drug (ID: DM21WBH)

Drug Name
MK-2461 Drug Info
Synonyms MK 2461
Indication
Disease Entry ICD 11 Status REF
Alzheimer disease 8A20 Phase 1/2 [1]
Cross-matching ID
PubChem CID
44137946
ChEBI ID
CHEMBL1822792
CAS Number
CAS 917879-39-1
TTD Drug ID
DM21WBH

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Investigative Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Anti-RON receptor mabs DMXACM2 Solid tumour/cancer 2A00-2F9Z Investigative [3]
ABC-7 DM2AIE9 Solid tumour/cancer 2A00-2F9Z Investigative [3]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fruquintinib DMHOSCQ Colorectal cancer 2B91.Z Approved [4]
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [5]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [6]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [7]
PI-88 DMGZPX6 Hepatocellular carcinoma 2C12.02 Phase 3 [8]
Taberminogene vadenovec DMW5PHL Vascular restinosis BE2Z Phase 3 [9]
ABT-869 DMREDYP Solid tumour/cancer 2A00-2F9Z Phase 3 [10]
MGCD516 DM752PU Solid tumour/cancer 2A00-2F9Z Phase 2/3 [11]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [12]
VATALANIB DMY0UEQ Solid tumour/cancer 2A00-2F9Z Phase 2 [13]
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Drug(s) Targeting Proto-oncogene c-Met (MET)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [14]
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [15]
Amivantamab DMZ7AMY Non-small-cell lung cancer 2C25 Approved [16]
Capmatinib DMYCXKL Non-small-cell lung cancer 2C25.Y Approved [17]
Tepotinib DMUQ0E8 Non-small-cell lung cancer 2C25 Approved [18]
RG3638 DMTQJE0 Gastric adenocarcinoma 2B72 Phase 3 [19]
Savolitinib DMALFKX Renal cell carcinoma 2C90 Phase 3 [20]
Beperminogene perplasmid DM6RWBN Critical limb ischemia BD4Y Phase 3 [21]
Tivantinib DMNVP8Q Hepatocellular carcinoma 2C12.02 Phase 3 [22]
MGCD516 DM752PU Solid tumour/cancer 2A00-2F9Z Phase 2/3 [19]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [23]
Intedanib DMSTA36 Colorectal cancer 2B91.Z Approved [24]
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [25]
Infigratinib DMNKBEC Cholangiocarcinoma 2C12.10 Approved [26]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [6]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [7]
ARQ-087 DM02BVQ Intrahepatic cholangiocarcinoma 2C12.10 Phase 3 [27]
AZD4547 DM3827C Solid tumour/cancer 2A00-2F9Z Phase 2/3 [28]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [20]
AM-001 DMGVQI8 Actinic keratosis EK90.0 Phase 2 [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Entrectinib DMMPTLH Non-small-cell lung cancer 2C25 Approved [30]
Larotrectinib DM26CQR Solid tumour/cancer 2A00-2F9Z Approved [31]
Altiratinib DMUJCBT Solid tumour/cancer 2A00-2F9Z Phase 1 [32]
PMID28270021-Compound-WO2016054807Example1 DMD5QEL Chronic pain MG30 Patented [33]
PMID28270010-Compound-Figure24-b DM0QHLK N. A. N. A. Patented [32]
Pyrrolo[2,3-d]pyrimidine derivative 4 DME0WSR Chronic pain MG30 Patented [33]
3-amino-5-benzyl-substituted indazole derivative 1 DMFDURZ Chronic pain MG30 Patented [33]
PMID28270010-Compound-Figure5-1 DM2YAPJ N. A. N. A. Patented [32]
PMID28270021-Compound-WO2015042088Example4 DM6KXOQ Chronic pain MG30 Patented [33]
PMID28270010-Compound-Figure5-2 DMK3GRZ N. A. N. A. Patented [32]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
ONO-7475 DMV6GX7 Acute leukaemia 2A60 Phase 1/2 [20]
ONO-7475 DMV6GX7 Acute leukaemia 2A60 Phase 1/2 [34]
RXDX-106 DM6NVTR Solid tumour/cancer 2A00-2F9Z Phase 1 [35]
MRX-2843 DMM5N8P Solid tumour/cancer 2A00-2F9Z Phase 1 [36]
PF-07265807 DMSMNRQ Solid tumour/cancer 2A00-2F9Z Phase 1 [37]
INCB81776 DMFOXGB Solid tumour/cancer 2A00-2F9Z Phase 1 [38]
LDC1267 DMH7R6L Discovery agent N.A. Investigative [39]
G749 DMC7HIS Discovery agent N.A. Investigative [40]
UNC2025 DMCU59W Glioblastoma of brain 2A00.00 Investigative [41]
UNC569 DMJL6ZM Acute lymphoblastic leukaemia 2A85 Investigative [42]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [25]
Interferon Alfa-2a, Recombinant DMUTZ8S Chronic HCV-1 infection 1E51.1 Approved [43]
Palifermin DM9JOYP Oral mucositis DA01.11 Approved [44]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [6]
Trafermin DMLKI2B Periodontitis DA0C Phase 3 [45]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [20]
LY2874455 DMZ0DMY Solid tumour/cancer 2A00-2F9Z Phase 2 [46]
AEE-788 DMEOS5K Solid tumour/cancer 2A00-2F9Z Phase 1/2 [47]
BAY1179470 DM7L91K Solid tumour/cancer 2A00-2F9Z Phase 1 [48]
Alofanib DMIEKTF Gastric adenocarcinoma 2B72 Phase 1 [49]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [50]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [51]
Becaplermin DM1R5X4 Diabetic complication 5A2Y Approved [52]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [6]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [12]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [53]
SNN-0031 DM2X3BR Brain injury NA07.Z Phase 1/2 [54]
TAK-593 DMNFZOT Solid tumour/cancer 2A00-2F9Z Phase 1 [55]
Pyridine derivative 18 DMBZMYT N. A. N. A. Patented [56]
PMID25656651-Compound-21a DMCKAON N. A. N. A. Patented [57]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [58]
Ponatinib DMYGJQO Acute lymphoblastic leukaemia 2A85 Approved [14]
Intedanib DMSTA36 Colorectal cancer 2B91.Z Approved [24]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [47]
Gilteritinib DMTI0ZO Acute myeloid leukaemia 2A60 Approved [31]
Pexidartinib DMS2J0Z Tenosynovial giant cell tumour 2F7B Approved [59]
Pacritinib DM1T6ZN Myelofibrosis 2A20.2 Approved [58]
Quizartinib DM8Y4JS Acute myeloid leukaemia 2A60 Approved [20]
Lestaurtinib DMQ2AIJ Acute myeloid leukaemia 2A60 Approved (orphan drug) [60]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [12]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [61]
VATALANIB DMY0UEQ Solid tumour/cancer 2A00-2F9Z Phase 2 [62]
Sirna-027 DMZTQD8 Exudative age-related macular degeneration 9B78.3Z Phase 1/2 [63]
PMID22765894C8h DMH5RFU Discovery agent N.A. Investigative [64]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole DM0CSH8 Discovery agent N.A. Investigative [65]
AAL-993 DM35RFH Discovery agent N.A. Investigative [62]
PMID17935989C25 DML8ZBR Discovery agent N.A. Investigative [66]
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile DMX6QMT Discovery agent N.A. Investigative [13]
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide DMI3OR9 Discovery agent N.A. Investigative [67]
(2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine DMQWD75 Discovery agent N.A. Investigative [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [50]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [23]
Regorafenib DMHSY1I Gastrointestinal stromal tumour 2B5B Approved [14]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [68]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [69]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [47]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [70]
Fruquintinib DMHOSCQ Colorectal cancer 2B91.Z Approved [4]
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [15]
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [5]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Entrectinib DMMPTLH Non-small-cell lung cancer 2C25 Approved [30]
Larotrectinib DM26CQR Solid tumour/cancer 2A00-2F9Z Approved [31]
PMID28270021-Compound-WO2016054807Example1 DMD5QEL Chronic pain MG30 Patented [33]
PMID28270010-Compound-Figure24-b DM0QHLK N. A. N. A. Patented [32]
Pyrrolo[2,3-d]pyrimidine derivative 4 DME0WSR Chronic pain MG30 Patented [33]
3-amino-5-benzyl-substituted indazole derivative 1 DMFDURZ Chronic pain MG30 Patented [33]
PMID28270010-Compound-Figure5-1 DM2YAPJ N. A. N. A. Patented [32]
PMID28270021-Compound-WO2015042088Example4 DM6KXOQ Chronic pain MG30 Patented [33]
PMID28270010-Compound-Figure5-2 DMK3GRZ N. A. N. A. Patented [32]
PMID28270010-Compound-Figure5-3 DMSOT1R N. A. N. A. Patented [32]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [25]
Trapidil DMY67U8 Acute coronary syndrome BA41 Phase 4 [71]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [6]
TKI258 DMYLT67 Renal cell carcinoma 2C90 Phase 3 [47]
BMS-582664 DMDAN8H Hepatocellular carcinoma 2C12.02 Phase 3 [47]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [20]
B-701 DMOMDA4 Bladder cancer 2C94 Phase 2 [72]
Recifercept DML8N3Y Achondroplasia LD24.00 Phase 2 [73]
AEE-788 DMEOS5K Solid tumour/cancer 2A00-2F9Z Phase 1/2 [47]
Anti-FGFR3 DM6QENU Multiple myeloma 2A83 Phase 1 [74]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [75]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [76]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [77]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [78]
Folic Acid DMEMBJC Colorectal carcinoma Approved [79]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [80]
Menadione DMSJDTY Vitamin K deficiency 5B59 Approved [81]
Arsenic DMTL2Y1 N. A. N. A. Approved [82]
Vorinostat DMWMPD4 Adult acute monocytic leukemia Approved [83]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [84]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [85]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [86]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [87]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [88]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [89]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [90]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [91]
Gefitinib DM15F0X Colon adenocarcinoma Approved [92]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [93]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [94]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [95]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [86]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [96]
Paclitaxel DMLB81S Breast carcinoma Approved [97]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [98]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [85]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [99]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [100]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [88]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [89]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
BDNF/NT-3 growth factors receptor (TrkB) TTKN7QR NTRK2_HUMAN Inhibitor [1]
Fibroblast growth factor receptor 1 (FGFR1) TTRLW2X FGFR1_HUMAN Inhibitor [1]
Fibroblast growth factor receptor 2 (FGFR2) TTGJVQM FGFR2_HUMAN Inhibitor [1]
Fibroblast growth factor receptor 3 (FGFR3) TTST7KB FGFR3_HUMAN Inhibitor [1]
Fms-like tyrosine kinase 3 (FLT-3) TTGJCWZ FLT3_HUMAN Inhibitor [1]
Macrophage-stimulating protein receptor (RON) TTBQ3OC RON_HUMAN Inhibitor [1]
NT-3 growth factor receptor (TrkC) TTXABCW NTRK3_HUMAN Inhibitor [1]
Platelet-derived growth factor receptor beta (PDGFRB) TTI7421 PGFRB_HUMAN Inhibitor [1]
Proto-oncogene c-Met (MET) TTNDSF4 MET_HUMAN Inhibitor [1]
Tyrosine-protein kinase Mer (MERTK) TTO7LKR MERTK_HUMAN Inhibitor [1]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Inhibitor [1]
Vascular endothelial growth factor receptor 3 (FLT-4) TTDCBX5 VGFR3_HUMAN Inhibitor [1]
VEGFR1 messenger RNA (VEGFR1 mRNA) TT1VAUK VGFR1_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
High affinity nerve growth factor receptor (NTRK1) OTJORQAU NTRK1_HUMAN Gene/Protein Processing [2]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Post-Translational Modifications [2]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Post-Translational Modifications [2]

References

1 MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
2 Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. J Med Chem. 2011 Jun 23;54(12):4092-108. doi: 10.1021/jm200112k. Epub 2011 May 24.
3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1816).
4 Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
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8 Company report (Medigen)
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12 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
13 Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9.
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16 Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209.
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20 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
21 Beperminogene perplasmid for the treatment of critical limb ischemia. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1145-56.
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28 AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
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32 Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
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38 A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity. Front Oncol. 2020 Dec 7;10:598477.
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40 G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19.
41 MerTK as a therapeutic target in glioblastoma. Neuro Oncol. 2018 Jan 10;20(1):92-102.
42 UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol Cancer Ther. 2013 Nov;12(11):2367-77.
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47 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
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59 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
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61 New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
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64 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
65 Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9.
66 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and prelimina... Bioorg Med Chem Lett. 2007 Dec 1;17(23):6593-601.
67 Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. J Med Chem. 2004 Oct 21;47(22):5367-80.
68 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
69 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
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71 Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
72 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
73 In vitro and in vivo characterization of Recifercept, a soluble fibroblast growth factor receptor 3, as treatment for achondroplasia. PLoS One. 2020 Dec 28;15(12):e0244368.
74 Clinical pipeline report, company report or official report of Genentech (2011).
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