ライフサイエンスコーパス: first-in-class

1 logy drugs were more likely to be orphan and first in class.

2 Ezetimibe is the first in class 2-azetidinone that decreases plasma chole

3 b (Velcade, PS341) was licensed in 2003 as a first-in-class 20S proteasome inhibitor indicated for tr

4 Herein, we report the development of 2 first-in-class (89)Zr-labeled PET tracers that enable th

5 The small molecules described here represent first-in-class activators of PKM2.

6 e and postoperative infusion of acadesine, a first-in-class adenosine-regulating agent, was associate

7 This first-in-class agent, with its novel mechanism of action

8 r-binding OR, and in addition, demonstrate a first-in-class agonist to further research in insect OR

9 Varlilumab is a novel, first-in-class, agonist CD27 antibody that stimulates th

10 mpound 1 is a candidate for development as a first-in-class analgesic.

11 Brentuximab vedotin, first in class and gold standard, was chosen for a proof

12 new oncology drug approvals were more often first-in-class and diffused more widely across important

13 ssessed the efficacy and safety of LCZ696, a first-in-class angiotensin receptor neprilysin inhibitor

14 Orencia is the first-in-class antagonist of CD28 costimulation.

15 ent of Cubicin (daptomycin-for-injection), a first-in-class antibiotic approved for treatment of skin

16 Rovalpituzumab tesirine is a first-in-class antibody-drug conjugate directed against

17 AS1411 is a first-in-class anticancer agent, currently in phase II c

18 ated the efficacy and safety of vosaroxin, a first-in-class anticancer quinolone derivative, plus cyt

19 Retigabine (RTG) is a first-in-class antiepileptic drug that suppresses neuron

20 Gal-B2 may lead to development of first-in-class antiepileptic drugs.

21 ONC201/TIC10 is a first-in-class antitumor agent that induces TRAIL pathwa

22 We previously discovered first-in-class beta-arrestin-biased agonists of dopamine

23 s further increases bone mass, we engineer a first-in-class bispecific antibody with single residue p

24 are now being realized with the approval of first-in-class BRCA-targeted therapies for ovarian cance

25 This first-in-class caspase inhibitor is now the subject of t

26 Here, we report the development of first-in-class cell-penetrating lipopeptide "pepducin" a

27 These studies provide a first-in-class chemical probe to study SCA10 RNA toxicit

28 d a new understanding of immunity, enabled a first-in-class clinical trial using bioelectronic device

29 mia (CML) cell lines with commercial and the first-in-class clinical WEE1 kinase inhibitor MK1775 con

30 Belatacept is a first-in-class co-stimulation blocker in development for

31 The recent approval of eculizumab as a first-in-class complement inhibitor for the treatment of

32 d plasma, and more potent, compared with the first-in-class compound ferrostatin-1 (Fer-1).

33 Therefore, CD-160130 is a promising first-in-class compound to attempt oncologic therapy wit

34 Elesclomol, an investigational first-in-class compound, induces oxidative stress, trigg

35 ng new drugs to inhibit viruses resistant to first-in-class compounds.

36 oline tetrathiomolybdate (WTX101) is an oral first-in-class copper-protein-binding molecule that targ

37 These first-in-class covalent K-Ras inhibitors demonstrate tha

38 better selectivity index and represents the first-in-class DENV-NS5 allosteric inhibitor able to tar

39 ith the desired functionality, including the first-in-class devices including sensors and memristors,

40 lpituzumab teserine (Rova-T; SC16LD6.5) is a first-in-class DLL3-targeted antibody-drug conjugate wit

41 iomarkers for treatment with AsiDNA, a novel first-in-class DNA repair inhibitor.

42 tured bacteria, is considered as a promising first-in-class drug candidate for clinical development.

43 dentification of DNDI-VL-2098 as a potential first-in-class drug candidate for visceral leishmaniasis

44 We identified the first-in-class drug candidates that transiently sequeste

45 Recent reports of new chemical entities and first-in-class drug candidates, and confirmation of indi

46 Tocilizumab is the first-in-class drug developed to treat diseases mediated

47 d and Drug Administration-approved Picato, a first-in-class drug for the treatment of the precancerou

48 f HIV-infected patients with nevirapine, the first-in-class drug still widely used, especially in dev

49 d in EAE and that laquinimod may represent a first-in-class drug targeting AhR for the treatment of m

50 cancer treatment through the development of "first-in-class" drugs that target oncogenic coactivators

51 in the 2014 FDA approval of suvorexant as a first-in-class dual orexin receptor antagonist for the t

52 MLN4924 is a first-in-class experimental cancer drug that inhibits th

53 motif, which results in pharmacology that is first-in-class for the central melanocortin receptors.

54 C3 is a first-in-class functionalized water-soluble fullerene th

55 This effort represents the discovery of first-in-class GAB1 PH domain inhibitors with potential

56 flunarizine and related compounds represent first-in-class HCV fusion inhibitors that merit consider

57 Vismodegib, a first-in-class Hedgehog-pathway inhibitor, is approved f

58 The discovery and development of the first-in-class hepatitis C virus (HCV) NS5A replication

59 PT2385 is a first-in-class HIF-2alpha antagonist.

60 he C-3' dimethyl group of bevirimat (2), the first-in-class HIV maturation inhibitor, which is curren

61 Ipilimumab is the first-in-class immunotherapeutic for blockade of CTLA-4

62 of this analysis, we have investigated which first in class inhibitor that entered phase I clinical t

63 However, MNKI-85, a first-in-class inhibitor of Mnk2, can be used as a power

64 identified as a potent, orally bioavailable first-in-class inhibitor of orthopoxvirus egress from in

65 evaluated selinexor, an orally bioavailable, first-in-class inhibitor of the nuclear export protein X

66 AZD1775 is a first-in-class inhibitor of Wee1 kinase with single-agen

67 the small molecule SBI-0640756 (SBI-756), a first-in-class inhibitor that targets eIF4G1 and disrupt

68 Ceapins are first-in-class inhibitors that can be used to explore bo

69 We report the development of a first-in-class intracellular PAR1 inhibitor with optimiz

70 identification of CP-690,550 1, a potential first-in-class JAK inhibitor for treatment of autoimmune

71 Analysis of the target validation history of first in class kinase inhibitors revealed a long delay b

72 This first-in-class macrocyclic peptide modulator of the hedg

73 The first-in-class maturation inhibitor bevirimat (BVM) fail

74 and humans, making NOX4 a prime target for a first-in-class mechanism-based, cytoprotective therapy i

75 Discovery of first-in-class medicines for treating cancer is limited

76 Eculizumab, a first-in-class monoclonal antibody that inhibits termina

77 We used a first-in-class, monoclonal antibody (MABp1) cloned from

78 Ibalizumab (formerly TNX-355) is a first-in-class, monoclonal antibody inhibitor of CD4-med

79 On the basis of these findings, a first-in-class MUC1-C inhibitor has entered phase I eval

80 Daily treatment of rats with the first-in-class NAMPT stimulator, P7C3-A20, prevented beh

81 Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception

82 ies support the further optimization of this first-in-class NOTCH1 inhibitor with dual selectivity: l

83 rt the development and characterization of a first-in-class novel azole analog [1-(4-(4-(((2R,4S)-2-(

84 Compound 71 is a first-in-class nucleoside RSV polymerase inhibitor that

85 eft ventricular dysfunction and could be the first in class of a new therapeutic agent.

86 Idelalisib is a first-in-class oral inhibitor of PI3Kdelta that has show

87 We aimed to investigate the efficacy of a first-in-class oral P2X3 antagonist, AF-219, to reduce c

88 pharmacodynamics of ibrutinib (PCI-32765), a first-in-class, oral covalent inhibitor of BTK designed

89 AQX-1125 is a first-in-class, oral SHIP1 activator with a novel anti-i

90 Enasidenib (AG-221/CC-90007) is a first-in-class, oral, selective inhibitor of mutant-IDH2

91 Eltrombopag (SB-497 115) is a first-in-class, oral, small-molecule, nonpeptide agonist

92 its continued development as a LANCL2-based, first-in-class orally active therapeutic for IBD.

93 Compound 2 represents a first-in-class, orally bioavailable, novel compound that

94 dioides species that is being developed as a first-in-class orphan product for treatment of coccidioi

95 MTI-101 is a first-in-class peptidomimetic that binds a CD44/ITGA4 co

96 re-based drug design effort that led to this first-in-class pharmacologic agent.

97 chemical biology labs interested in creating first-in-class pharmacological probes for challenging pr

98 y of [(11)C]-(R)-3 ([(11)C]-(R)-IPMICF16), a first-in-class positron emission tomography (PET) TrkB/C

99 Here, we report the discovery of (R)-PFI-2-a first-in-class, potent (Ki (app) = 0.33 nM), selective,

100 Purpose AZD1775 is a first-in-class, potent, and selective inhibitor of WEE1

101 First in class, priority review, fast track, orphan drug

102 onse rates of AL amyloidosis patients to the first-in-class proteasome inhibitor (PI) bortezomib, we

103 se 1 trials of bortezomib 10 years ago, this first-in-class proteasome inhibitor (PI) has contributed

104 rch & Development, L.L.C., Raritan, NJ) is a first-in-class proteasome inhibitor developed specifical

105 Bortezomib is a first in class proteosomal inhibitor, that is Food and D

106 We examined the potential of a first-in-class radiofluorinated small-molecule inhibitor

107 r therapy with the approval of bortezomib, a first-in-class, reversible proteasome inhibitor, for rel

108 eported for a kinase ribozyme, making this a first-in-class ribozyme.

109 Here we show that HDAC3 inhibition using a first in class selective inhibitor, RGFP966, resulted in

110 We previously reported that a first-in-class selective class IIa histone deacetylase (

111 First-in-class selective PET tracers for imaging VEGFR-1

112 Selinexor is a novel, first-in-class, selective inhibitor of nuclear export co

113 L as a versatile reactive group for creating first-in-class serine hydrolase inhibitors.

114 Herein, we report on the discovery of first-in-class small molecule compounds that inhibit the

115 The first-in-class small molecule inhibitor OTX015 (MK-8628)

116 Further, we developed a first-in-class small molecule inhibitor toward FIEL1 tha

117 represents, to the best of our knowledge, a first-in-class small molecule that exerts a probe-depend

118 This first-in-class small-molecule activator targeting SERCA2

119 Our approach is the first to identify a first-in-class small-molecule antagonist of activin bind

120 ither RNA interference or, to our knowledge, first-in-class small-molecule inhibitors of PU.1 that we

121 thy volunteer Phase 1 trials, making it the "first-in-class" small-molecule LOXL2 inhibitor to enter

122 We have identified a first-in-class, small molecule inhibitor of the eukaryot

123 CUDC-907 is an oral, first-in-class, small molecule that is designed to inhib

124 A phase 1 study of vismodegib (GDC-0449), a first-in-class, small-molecule inhibitor of the hedgehog

125 We developed a first-in-class, small-molecule PRMT5 inhibitor that bloc

126 The first-in-class soluble guanylate cyclase (sGC) stimulato

127 vemurafenib (RG7204; PLX4032; RO5185426), a first-in-class, specific small molecule inhibitor of BRA

128 oval times, clinical approval success rates, first-in-class status, and global market diffusion.

129 ned in the presence of either abiraterone, a first-in-class steroidal inhibitor recently approved by

130 we report the crystal structures of TYK2, a first in class structure, and JAK3 in complex with PAN-J

131 This first-in-class study evaluated the anti-cholestatic effe

132 This first-in-class study supports further investigation of F

133 Overall, sulfated coumarins represent first-in-class, sub-maximal inhibitors of thrombin.

134 [(11)C]AZ12204657 is a first-in-class surrogate imaging biomarker for pancreati

135 efficacy and safety of adding idelalisib, a first-in-class targeted phosphoinositide-3-kinase delta

136 extra terminal protein (BET) inhibitors are first-in-class targeted therapies that deliver a new the

137 for the clinical development of CAL-101 as a first-in-class targeted therapy for CLL and related B-ce

138 HCC, a novel molecular target in SDH, and a first-in-class therapy to treat the disease.

139 To surmount these challenges, we created a first-in-class, tri-part split luciferase consisting of

140 ture of RAP1/TRF2 complex, we have developed first-in-class triazole-stapled peptides that block the

141 We show that pazopanib is the first-in-class VEGF receptor inhibitor to inhibit in viv

142 It is currently in a clinical trial as a first in class, VEGFr2 targeting, topically applied comp