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1 logy drugs were more likely to be orphan and first in class.
3 b (Velcade, PS341) was licensed in 2003 as a first-in-class 20S proteasome inhibitor indicated for tr
4 ere we show the properties of analogues of a first-in-class 4R-tau lead, [(18)F]OXD-2115, using ligan
7 e and postoperative infusion of acadesine, a first-in-class adenosine-regulating agent, was associate
10 r-binding OR, and in addition, demonstrate a first-in-class agonist to further research in insect OR
12 cacy of rentosertib (formerly ISM001-055), a first-in-class AI-generated small-molecule inhibitor of
16 assess efficacy and safety of firibastat, a first-in-class aminopeptidase A inhibitor preventing con
19 these studies highlighted compound 31 as the first-in-class and a suitable candidate for in vivo prec
20 new oncology drug approvals were more often first-in-class and diffused more widely across important
21 ssessed the efficacy and safety of LCZ696, a first-in-class angiotensin receptor neprilysin inhibitor
24 pendent cell cytotoxicity using lacutamab, a first-in-class anti-KIR3DL2 humanized antibody, selectiv
25 been reported.Sacituzumab govitecan (SG), a first-in-class anti-trophoblast cell surface antigen 2 (
26 ent of Cubicin (daptomycin-for-injection), a first-in-class antibiotic approved for treatment of skin
28 Designed sustainably to deliver novel and first-in-class antibiotics targeting key human health ga
33 ated the efficacy and safety of vosaroxin, a first-in-class anticancer quinolone derivative, plus cyt
40 and preclinical characterization of CD388, a first-in-class antiviral drug-Fc conjugate (DFC), in mic
42 phase III trial suggest that plitidepsin, a first-in-class antiviral, may have a positive benefit-ri
43 ds was affected by the drug fulvestrant, the first-in-class approved selective estrogen receptor degr
47 leveraged for the therapeutic development of first-in-class BET inhibitors and other targeted strateg
52 s further increases bone mass, we engineer a first-in-class bispecific antibody with single residue p
53 he metabolic liabilities of PQR620 (52), the first-in-class brain penetrant TORKi showing efficacy in
54 are now being realized with the approval of first-in-class BRCA-targeted therapies for ovarian cance
56 ess the efficacy and safety of mavacamten, a first-in-class cardiac myosin inhibitor, in symptomatic
58 on of STM2457, a highly potent and selective first-in-class catalytic inhibitor of METTL3, and a crys
64 d a new understanding of immunity, enabled a first-in-class clinical trial using bioelectronic device
65 mia (CML) cell lines with commercial and the first-in-class clinical WEE1 kinase inhibitor MK1775 con
75 oline tetrathiomolybdate (WTX101) is an oral first-in-class copper-protein-binding molecule that targ
76 roved BTK inhibitors, including Ibrutinib, a first-in-class covalent inhibitor of BTK, bind directly
80 roader application of KPT-330 (selinexor), a first-in-class CRM1 inhibitor recently approved for rela
81 anced to clinical development as a potential first-in-class D1 PAM and is now in phase 2 studies for
83 ged PROTAC strategy, we discovered MS28, the first-in-class degrader of cyclin D1, which lacks a smal
85 better selectivity index and represents the first-in-class DENV-NS5 allosteric inhibitor able to tar
86 areas, modalities, route of administration, first-in-class designation, approval times, and expedite
87 ith the desired functionality, including the first-in-class devices including sensors and memristors,
89 t and orthogonal counterscreens identified a first-in-class direct-acting RABV inhibitor, GRP-60367,
90 lpituzumab teserine (Rova-T; SC16LD6.5) is a first-in-class DLL3-targeted antibody-drug conjugate wit
94 tured bacteria, is considered as a promising first-in-class drug candidate for clinical development.
95 dentification of DNDI-VL-2098 as a potential first-in-class drug candidate for visceral leishmaniasis
97 Recent reports of new chemical entities and first-in-class drug candidates, and confirmation of indi
100 d and Drug Administration-approved Picato, a first-in-class drug for the treatment of the precancerou
101 f HIV-infected patients with nevirapine, the first-in-class drug still widely used, especially in dev
102 d in EAE and that laquinimod may represent a first-in-class drug targeting AhR for the treatment of m
104 edict ligands from virtual libraries yielded first-in-class, drug-like ligands for 7 of the 16 WDR do
105 he basis for the development of IDO1 PAMs as first-in-class drugs in autoimmune/neuroinflammatory dis
106 rugs, products in certain therapeutic areas, first-in-class drugs, therapeutic agents that received a
107 market, such as accelerating approval of non-first-in-class drugs, will likely not result in lower dr
108 cancer treatment through the development of "first-in-class" drugs that target oncogenic coactivators
110 and-directed degrader targeting the AR via a first-in-class dual mechanism of AR degradation and anta
111 in the 2014 FDA approval of suvorexant as a first-in-class dual orexin receptor antagonist for the t
113 ting EGFR degrader, MS39 (compound 6), and a first-in-class E3 ligase cereblon-recruiting EGFR degrad
114 e emergence of new technologies coupled with first-in-class entries in ophthalmology are highly antic
116 study population, which ultimately supported first-in-class FDA clearance for extragenital assays.
118 like (MASTL) represents a novel target and a first-in-class (FIC) opportunity to provide a new impact
119 motif, which results in pharmacology that is first-in-class for the central melanocortin receptors.
123 The compounds reported herein represent a first-in-class genotype-selective series that specifical
124 essful third-generation approach leverages a first in class glycosylation of a phosphoglycerol-functi
125 flunarizine and related compounds represent first-in-class HCV fusion inhibitors that merit consider
131 port the discovery and characterization of a first-in-class, highly selective allosteric inhibitor of
132 ns and identified a chemically well-behaved, first-in-class hit with nanomolar anti-RABV potency that
133 he C-3' dimethyl group of bevirimat (2), the first-in-class HIV maturation inhibitor, which is curren
137 ty and tolerability of MOv18 IgE, a chimeric first-in-class IgE antibody, in patients with tumours ex
139 a highly attractive target for developing a first-in-class immunotherapy, albeit one with a potentia
140 of this analysis, we have investigated which first in class inhibitor that entered phase I clinical t
145 identified as a potent, orally bioavailable first-in-class inhibitor of orthopoxvirus egress from in
147 evaluated selinexor, an orally bioavailable, first-in-class inhibitor of the nuclear export protein X
150 the small molecule SBI-0640756 (SBI-756), a first-in-class inhibitor that targets eIF4G1 and disrupt
153 imes, and in vivo PK properties, to identify first-in-class inhibitors that demonstrate LDH inhibitio
154 raction Discovery and Exploration (SLIDE), a first-in-class interpretable machine learning technique
156 Fostemsavir is the prodrug of temsavir, a first-in-class investigational HIV-1 attachment inhibito
159 identification of CP-690,550 1, a potential first-in-class JAK inhibitor for treatment of autoimmune
161 Analysis of the target validation history of first in class kinase inhibitors revealed a long delay b
164 eukemic activity of this orally bioavailable first-in-class lysine-specific demethylase 1 inhibitor.
169 and humans, making NOX4 a prime target for a first-in-class mechanism-based, cytoprotective therapy i
171 These studies warrant identification of first-in-class MEIS inhibitors as potential pharmaceutic
173 , a specific antisense oligonucleotide, is a first-in-class miR-132 inhibitor that attenuates and eve
174 upport our discovery that roseltide rT1 is a first-in-class mitochondria-targeting, cysteine-rich pep
175 dent on ML-based TO assessment, we deliver a first-in-class ML-based target pharmacology assessment f
186 we report the discovery and development of a first-in-class non-covalent small-molecule inhibitor of
188 ies support the further optimization of this first-in-class NOTCH1 inhibitor with dual selectivity: l
189 rt the development and characterization of a first-in-class novel azole analog [1-(4-(4-(((2R,4S)-2-(
193 ng excitatory neurotransmission, providing a first-in-class optogenetic tool for persistent, light-tr
194 On the basis of the activity of duvelisib, a first-in-class oral dual inhibitor of phosphoinositide 3
196 We aimed to investigate the efficacy of a first-in-class oral P2X3 antagonist, AF-219, to reduce c
198 pharmacodynamics of ibrutinib (PCI-32765), a first-in-class, oral covalent inhibitor of BTK designed
199 d the activity and safety of tazemetostat, a first-in-class, oral EZH2 inhibitor, in patients with fo
205 characterization of ABBV-CLS-484 (AC484), a first-in-class, orally bioavailable, potent PTPN2 and PT
206 dioides species that is being developed as a first-in-class orphan product for treatment of coccidioi
207 reclinical studies, neladenoson bialanate, a first-in-class partial adenosine A1 receptor agonist, ha
210 se or oncology, and more than 10 potentially first-in-class peptide therapeutics are in the pipeline.
214 by recapitulating the phenotype using BT5, a first-in-class pharmacologic inhibitor against NSD1.
215 chemical biology labs interested in creating first-in-class pharmacological probes for challenging pr
217 y of [(11)C]-(R)-3 ([(11)C]-(R)-IPMICF16), a first-in-class positron emission tomography (PET) TrkB/C
219 Here, we report the discovery of (R)-PFI-2-a first-in-class, potent (Ki (app) = 0.33 nM), selective,
221 es, we advanced compound 9 to compound 15, a first-in-class, potent, selective, and bioavailable inhi
226 onse rates of AL amyloidosis patients to the first-in-class proteasome inhibitor (PI) bortezomib, we
227 se 1 trials of bortezomib 10 years ago, this first-in-class proteasome inhibitor (PI) has contributed
228 rch & Development, L.L.C., Raritan, NJ) is a first-in-class proteasome inhibitor developed specifical
232 red the safety and efficacy of mavacamten, a first-in-class reversible inhibitor of cardiac-specific
233 r therapy with the approval of bortezomib, a first-in-class, reversible proteasome inhibitor, for rel
235 Here we show that HDAC3 inhibition using a first in class selective inhibitor, RGFP966, resulted in
241 e the design, synthesis, and evaluation of a first-in-class set of 5- to 7-membered ether-linked and
242 iscovery and characterization of RGLS4326, a first-in-class, short oligonucleotide inhibitor of micro
243 y potent, selective, orally efficacious, and first-in-class SHP2 inhibitor currently in clinical tria
247 lography revealed that a potent, reversible, first-in-class small molecule inhibitor of the oncogenic
250 y and a structure-based design, we developed first-in-class small molecule inhibitors of the ASH1L SE
251 represents, to the best of our knowledge, a first-in-class small molecule that exerts a probe-depend
254 e discovery and characterization of PZL-A, a first-in-class small-molecule activator of mtDNA synthes
256 immunohistochemistry to evaluate a series of first-in-class small-molecule activators of PP2A (SMAPs)
257 Our approach is the first to identify a first-in-class small-molecule antagonist of activin bind
259 ither RNA interference or, to our knowledge, first-in-class small-molecule inhibitors of PU.1 that we
260 thy volunteer Phase 1 trials, making it the "first-in-class" small-molecule LOXL2 inhibitor to enter
264 A phase 1 study of vismodegib (GDC-0449), a first-in-class, small-molecule inhibitor of the hedgehog
269 vemurafenib (RG7204; PLX4032; RO5185426), a first-in-class, specific small molecule inhibitor of BRA
270 oval times, clinical approval success rates, first-in-class status, and global market diffusion.
271 ned in the presence of either abiraterone, a first-in-class steroidal inhibitor recently approved by
272 we report the crystal structures of TYK2, a first in class structure, and JAK3 in complex with PAN-J
278 he discovery and development of olpasiran, a first-in-class, synthetic, double-stranded, N-acetylgala
279 enerated small-molecule inhibitor of TNIK, a first-in-class target in idiopathic pulmonary fibrosis (
280 3-expressing cancer cells and is a potential first-in-class targeted alpha-therapy in advanced HCC.
282 efficacy and safety of adding idelalisib, a first-in-class targeted phosphoinositide-3-kinase delta
283 extra terminal protein (BET) inhibitors are first-in-class targeted therapies that deliver a new the
284 for the clinical development of CAL-101 as a first-in-class targeted therapy for CLL and related B-ce
285 RER-HCM is a phase 3 trial in oHCM testing a first-in-class, targeted strategy of myosin inhibition t
287 ntified a small molecule compound, C35, as a first-in-class TET inhibitor that specifically blocks th
288 dy AFM13 is an innate immune cell engager, a first-in-class, tetravalent antibody, designed to create
291 To surmount these challenges, we created a first-in-class, tri-part split luciferase consisting of
294 ture of RAP1/TRF2 complex, we have developed first-in-class triazole-stapled peptides that block the
295 tly granted tissue-agnostic approval for the first-in-class TRK inhibitor larotrectinib for patients
297 len-2-yl)benzo[d]oxazole (ezutromid, 1) is a first-in-class utrophin modulator that has been evaluate
299 It is currently in a clinical trial as a first in class, VEGFr2 targeting, topically applied comp