ライフサイエンスコーパス: oral bioavailability

1 ly focused on the improvement in potency and oral bioavailability.

2 po and an improved in vivo rat clearance and oral bioavailability.

3 l to improve the delivery of drugs with poor oral bioavailability.

4 erparts, severely limiting exposure time and oral bioavailability.

5 ype 2 with low oxidative metabolism but poor oral bioavailability.

6 31 with desirable potency, selectivity, and oral bioavailability.

7 ting its half-life, tissue distribution, and oral bioavailability.

8 d improved metabolic stability and increased oral bioavailability.

9 lity increase appears linked to the improved oral bioavailability.

10 bitor, is a promising therapeutic agent with oral bioavailability.

11 cy screen to rapidly identify compounds with oral bioavailability.

12 led to meet criteria required for sufficient oral bioavailability.

13 tive at low nanomolar concentrations and has oral bioavailability.

14 anced dissolution rate is vital to guarantee oral bioavailability.

15 in vivo, leading to rapid clearance and low oral bioavailability.

16 subsequent analogues suffered from a lack of oral bioavailability.

17 the physicochemical space for optimum human oral bioavailability.

18 ly due to poor in vivo stability and lack of oral bioavailability.

19 potency, selectivity, in vivo efficacy, and oral bioavailability.

20 ent on the physicochemical space to optimize oral bioavailability.

21 nhibitors with enhanced potency and improved oral bioavailability.

22 H in surfactant-independent fashion and good oral bioavailability.

23 ation of the compound in the rat showed good oral bioavailability.

24 needed to identify parameters that influence oral bioavailability.

25 vely high clearance in rat, resulting in low oral bioavailability.

26 MDA-MB-231 cancer cell line, and has a good oral bioavailability.

27 ich demonstrated the antitumor efficacy with oral bioavailability.

28 ity for the A(2B)-AdoR, as well as improving oral bioavailability.

29 t cellular potency (IC50 < 100 nM), and good oral bioavailability.

30 water and lipids and therefore can influence oral bioavailability.

31 retained factor Xa binding affinity and good oral bioavailability.

32 selective ROCK1 inhibitor but possessed poor oral bioavailability.

33 l role in decreasing clearance and improving oral bioavailability.

34 nds with excellent potency, selectivity, and oral bioavailability.

35 idazole DGAT1 inhibitor 1 led to 9 with good oral bioavailability.

36 2, and acetamides such as 3a,b exhibit poor oral bioavailability.

37 d and 5k that demonstrated no improvement in oral bioavailability.

38 xcellent drug-like properties including high oral bioavailability.

39 able, larger pentapeptides generally had low oral bioavailability.

40 elective CRTH2 antagonists that possess good oral bioavailability.

41 -life ranging from 91 to 127 minutes and 43% oral bioavailability.

42 lpha(v)beta(5) dual antagonist with improved oral bioavailability.

43 material can have a strong influence on PAH oral bioavailability.

44 and two carboxylates, severely limiting its oral bioavailability.

45 e and transparent delivery systems with high oral bioavailability.

46 limited due to their low solubility, and low oral bioavailability.

47 single dose administration showing favorable oral bioavailability.

48 electivity for cancer over normal cells, and oral bioavailability.

49 studies, including low clearances and decent oral bioavailability.

50 in a mouse model of infection, and have 100% oral bioavailability.

51 dried powders of itraconazole to enhance its oral bioavailability.

52 ffold and endowed with better solubility and oral bioavailability.

53 nimal toxicity against normal cells and good oral bioavailability.

54 cation of 23 as an attractive lead with good oral bioavailability.

55 a disulfide bond with side chains improving oral bioavailability.

56 nd low efflux, suggesting high potential for oral bioavailability.

57 luble and consequently have unacceptably low oral bioavailabilities.

58 d phosphonate prodrugs of 10A exhibited poor oral bioavailability (0.2-11%).

59 two rodent pain models, 1 suffered from low oral bioavailability (18%) and moderate hERG channel inh

60 Improved oral bioavailability (22-47%) was achieved using phospho

61 zine (8a-b) led to a dramatic improvement in oral bioavailability (38-61%F) while maintaining the pot

62 y in the CFR (ED(50) 0.4 mg/kg, po) and good oral bioavailability (40%, rat) and was selected for dev

63 (human cathepsin K, K(i,app) = 0.16 nM, rat oral bioavailability = 42%, rat in vivo clearance = 49.2

64 he rat indicated that this compound has good oral bioavailability (51% at 20 mg/kg) and a reasonable

65 Compound 16g also shows good oral bioavailability (59%) and exhibits a brain/plasma r

66 t and selective nNOS inhibitor with improved oral bioavailability (60%) and no hERG channel inhibitio

67 -AUCB, IC50 = 1.3 +/- 0.05 nM) had excellent oral bioavailability (98%, n = 2) and blood area under t

68 otype member of this class (8) displays high oral bioavailability, access to the central nervous syst

69 selective compound (31) exhibiting favorable oral bioavailability across a range of preclinical speci

70 0b, AZD9496), a clinical candidate with high oral bioavailability across preclinical species that is

71 g through Lipinski's rule of five filter for oral bioavailability, ADMET risk filter for drug like fe

72 good pharmacokinetic profile in the rat (33% oral bioavailability after a 3 mg/kg dose, reaching a pe

73 ulfonyl hydrazide 40, which demonstrated 59% oral bioavailability and 73% of tumor growth delay witho

74 -isobutyryl prodrug of 2c, demonstrated good oral bioavailability and a high level of 2c-TP in vivo.

75 monstrated that compound 35 showed promising oral bioavailability and a moderate oral half life and i

76 inetic studies in dog demonstrated excellent oral bioavailability and a t1/2 of 15 h.

77 Since tipifarnib displays high oral bioavailability and acceptable pharmacokinetic prop

78 ug of cidofovir, brincidofovir, has improved oral bioavailability and achieves higher intracellular c

79 app) = 0.041 nM vs human cathepsin K and 89% oral bioavailability and an in vivo clearance rate of 19

80 research designed to quantify the extent of oral bioavailability and bioaccessibility of organic and

81 mum is recommended for future studies on the oral bioavailability and bioaccessibility of PAHs in soi

82 Compound 30 showed good oral bioavailability and brain penetration across specie

83 33 has good stability and oral bioavailability and can cross the blood-brain barri

84 talytic OP bioscavenger with the prospect of oral bioavailability and central nervous system penetrat

85 he inhibitors currently in development limit oral bioavailability and clinical development.

86 ossess chemical properties more conducive to oral bioavailability and CNS penetration.

87 still has some issues including solubility, oral bioavailability and cost of preparation.

88 For both the oral bioavailability and dermal absorption studies, the

89 Compound 5 has a good oral bioavailability and effectively inhibits tumor grow

90 racils are potent GnRH antagonists with good oral bioavailability and efficacy in nonhuman primates.

91 In rodent, the compound displays high oral bioavailability and excellent brain penetration aff

92 Concomitant benefits are good oral bioavailability and high plasma concentrations in v

93 pound 14a (hTRPV1 IC50 = 4 nM) exhibited 46% oral bioavailability and in vivo activity in animal mode

94 Quinoline 16 showed good oral bioavailability and in vivo efficacy in a LDLr knoc

95 BJ486K has oral bioavailability and interferes with entry of HCV in

96 and dog with respect to plasma clearance and oral bioavailability and is a potent inhibitor in vivo o

97 a promising drug delivery system to improve oral bioavailability and lipid-lowering effect of PB.

98 onist with an ED50 = 2.3 mg/kg in rats, high oral bioavailability and low-moderate clearance in precl

99 anshinones in micronized GP of SM had higher oral bioavailability and lower individual variances, thu

100 ified compound 10b, which displayed improved oral bioavailability and lower intrinsic clearance.

101 nously expressed CRTH2, 5) demonstrates good oral bioavailability and metabolic stability in various

102 ofimilast), a potent PDE4 inhibitor with low oral bioavailability and no emesis-associated behaviors

103 wild-type and key mutant viruses, excellent oral bioavailability and overall pharmacokinetics, and a

104 licon cells, and exhibited consistently high oral bioavailability and pharmacokinetic parameters acro

105 They have good oral bioavailability and pharmacokinetics and induced co

106 ns, its well characterized activity profile, oral bioavailability and pharmacological properties indi

107 This work aimed to improve the oral bioavailability and plasma lipid-lowering effect of

108 ofile of some of these analogues showed >25% oral bioavailability and po half-lives of at least 1.5 h

109 the biaryl and N-arylpiperazine analogues by oral bioavailability and potency.

110 In animals, 10d showed moderate to good oral bioavailability and promoted food intake in tumor-b

111 ts for one carboxamide analogue demonstrated oral bioavailability and reasonable in vivo clearance.

112 tification of potent compounds with improved oral bioavailability and reduced cardiac ion channel lia

113 es such as the TTR amyloidoses include known oral bioavailability and safety data.

114 lin-resistant (MRSA) strains, low clearance, oral bioavailability and shows efficacy in a mouse neutr

115 INCB3344 possesses good oral bioavailability and systemic exposure in rodents th

116 he pharmacological potential of TCMPs, their oral bioavailability and their resistance to industrial

117 ABT-888 demonstrated good oral bioavailability and was well tolerated.

118 , compounds of the present class showed good oral bioavailability and were highly active in a standar

119 o demonstrate good pharmacokinetic profiles, oral bioavailability, and activity in vivo in an SW620 c

120 tabolic stability and permeability, complete oral bioavailability, and appreciable efficacy on glucos

121 ies have good in vitro ADME properties, good oral bioavailability, and efficacy after oral delivery i

122 flux in a Caco-2 assay, suggesting potential oral bioavailability, and exhibited minimal off-target b

123 le, high free fraction in human plasma, good oral bioavailability, and in vivo efficacy in antithromb

124 penetration, lack of CYP450 inhibition, high oral bioavailability, and pharmacokinetic properties.

125 The compound has approximately 70% oral bioavailability, and pharmacologic studies using bo

126 te its potency, Rapa has low solubility, low oral bioavailability, and rapid systemic clearance, whic

127 compounds with increased potency, excellent oral bioavailability, and robust efficacy in a murine mo

128 01), has medication-like duration of action, oral bioavailability, and target engagement.

129 highest plateau plasma PB concentration and oral bioavailability, and the greatest cholesterol-lower

130 e understanding of antitumor mechanisms, low oral bioavailability, and unpredictable pharmacokinetics

131 en receptor degrader (SERD), exhibiting good oral bioavailability, antitumor efficacy, and SERD activ

132 vity relationships and optimization of their oral bioavailability are presented.

133 itial studies of absorption, metabolism, and oral bioavailability are reported.

134 sides have increased metabolic stability and oral bioavailability as determined from in vitro PAMPA p

135 g its substrates and is believed to regulate oral bioavailability as well as serve a protective role

136 bstantially improved microsome stability and oral bioavailability, as well as in vivo activity.

137 e reviews the state of the science regarding oral bioavailability, bioaccessibility, and dermal absor

138 cles are administered orally, revealing that oral bioavailability can be obtained at molecular weight

139 logical profiles with significantly improved oral bioavailability compared to the well studied Aurora

140 ulfonamide (TL-77)] which has shown improved oral bioavailability compared with ON01910.Na.

141 is an anti-AIDS therapeutic agent with high oral bioavailability despite its high hydrophobicity.

142 Pharmacokinetic studies indicated that low oral bioavailability due to poor ADME properties.

143 1 and 2 displayed low plasma levels and poor oral bioavailability, due to rapid first-pass metabolism

144 In this study, PK parameters and absolute oral bioavailability expressed as percentage (F%) of cel

145 inyl analogues gave compounds with excellent oral bioavailability (F > 60%) when dosed in rat.

146 the range of 10-50 mg/kg, and exhibits good oral bioavailability (F = 39%).

147 in vitro and in vivo assays, exhibited good oral bioavailability (F = 42%, mesylate salt, rat) and r

148 rat CYP11B1 (IC50 = 2 muM) and showed a high oral bioavailability (F = 50%) and sufficient plasma con

149 lective CRF(1) receptor antagonist with good oral bioavailability (F = 52%) in rats and efficacy in t

150 es in rat led to compound 30, which has good oral bioavailability (F = 56%) and a favorable tissue di

151 However, its poor water solubility and low oral bioavailability (F) in rat suggested that the lead

152 Oral bioavailability (F) is a product of fraction absorb

153 D mouse model of P. falciparum malaria, good oral bioavailability, favorable enzyme selectivity, and

154 difluorinated compound versus essentially no oral bioavailability for the parent compound.

155 ) NOS isoforms and also showed potential for oral bioavailability (good cell permeability with efflux

156 high aqueous solubility (>30 mg/mL) and high oral bioavailability (>80% across species) that is curre

157 ater solubility, an optimal DMPK profile and oral bioavailability, halts SRC-associated neuromast mig

158 ar no small molecule inhibitors of CatA with oral bioavailability have been described to allow furthe

159 tabolism in human liver microsomes, and high oral bioavailability in animal models.

160 , is likely to be the major cause of its low oral bioavailability in humans (see the related article

161 use CCR3 (chemotaxis IC(50) = 41 nM) and its oral bioavailability in mice (20% F ) were adequate to a

162 adiazoles, afforded compounds with excellent oral bioavailability in mice (i.e., 50 F(po) = 79%).

163 Exemplary oral bioavailability in mice was achieved using the indo

164 orable in vitro ADME profile as well as good oral bioavailability in mice, rats, and dogs.

165 orted antiviral activity and established its oral bioavailability in mice.

166 Cyanopyrimidine 3a demonstrated 100% oral bioavailability in mouse.

167 favorable in vitro safety profiles and good oral bioavailability in mouse.

168 tly improved off-target activity profile and oral bioavailability in multiple species coupled with go

169 These compounds have excellent oral bioavailability in preclinical species and exhibit

170 ine specific serine proteases, and which has oral bioavailability in preclinical species and in vivo

171 Oral bioavailability in preclinical species ranged from

172 IC(50) = 6.3 nM) with excellent selectivity, oral bioavailability in preclinical species, and in vivo

173 ity over other proline-selective peptidases, oral bioavailability in preclinical species, and in vivo

174 In addition, 25f has 94% oral bioavailability in rat and >1000x selectivity over

175 compounds were identified that exhibit both oral bioavailability in rat and clinically relevant bact

176 Compound 8 has good oral bioavailability in rat and cynomolgus monkey, attra

177 cterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo eff

178 of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selec

179 avorable pharmacokinetic profiles and showed oral bioavailability in rat and dog.

180 Several of these analogues showed good oral bioavailability in rat and efficacy in the rat iodo

181 Compound 4 displayed good oral bioavailability in rat and may be a potential thera

182 several functional assays, showed excellent oral bioavailability in rat and monkey models, and showe

183 ing prodrug displayed only moderately higher oral bioavailability in rat than the polar direct thromb

184 esis model (ED50=0.01 mg/kg) as well as high oral bioavailability in rat, dog, and cynomolgus monkey.

185 ound 6b (ABT-670), which exhibited excellent oral bioavailability in rat, dog, and monkey (68%, 85%,

186 d promutagenic potential as well as very low oral bioavailability in rats (F = 2%) and was therefore

187 t potent of which (49a and 49b) exhibit good oral bioavailability in rats (F(oral) = 39% and 17%, res

188 Several analogs have also shown promising oral bioavailability in rats and cynomolgus monkey.

189 (3S,5R)-12 showed oral bioavailability in rats and demonstrated blood pres

190 o revealed that this molecule possesses good oral bioavailability in rats and effectively suppresses

191 ve in functional assays and showed excellent oral bioavailability in rats and monkeys.

192 s allowed us to identify analogues with good oral bioavailability in rats, dogs, and monkeys while th

193 d activity in functional assays and improved oral bioavailability in rats.

194 Antagonist 26 was shown to have good oral bioavailability in rats.

195 vitro (IC50 = 0.015 muM), which has moderate oral bioavailability in rodents and demonstrates robust

196 bits in vitro potency, cross-reactivity, and oral bioavailability in rodents, we evaluated the impact

197 metabolism, moderate permeability, and good oral bioavailability in rodents.

198 metabolism, moderate permeability, and good oral bioavailability in rodents.

199 manganic porphyrins for neuroprotection and oral bioavailability in the mouse 1-methyl-4-phenyl-1,2,

200 )Rs (rH(3)R K(i) = 8.5 nM) but displayed low oral bioavailability in the rat.

201 h favorable pharmacokinetics, including good oral bioavailability in the rat.

202 ns to the amide linkage can lead to improved oral bioavailability in this series.

203 parasite and were characterized by moderate oral bioavailability in vivo.

204 In rats, its oral bioavailability is 98% and it has a favorable plasm

205 Insufficient oral bioavailability is considered as a key limitation f

206 trating class I subtype selectivity and good oral bioavailability is described.

207 However, its low oral bioavailability is the major hurdle for moving this

208 ion model to rapidly identify compounds with oral bioavailability, leading to the discovery of severa

209 However, high instability and extremely low oral bioavailability limit its further clinical developm

210 Poor oral bioavailability limits the use of curcumin and othe

211 dely-studied lipophilic ingredients, but low oral bioavailability limits their clinical application.

212 Oral bioavailability, low off-target activity, favorable

213 d resistant parasites, moderate to excellent oral bioavailability, low toxicity in in vitro studies,

214 oor intrinsic solubility and low to moderate oral bioavailability made this series unsuitable for fur

215 The goal of this study was to determine if oral bioavailability mediates nonresponsiveness.

216 ing, with major hurdles in cell penetration, oral bioavailability/metabolic clearance, and brain acce

217 ctrum activity, a strong safety profile, and oral bioavailability, new discovery strategies must be i

218 se 1,6-bisphosphatase (FBPase) exhibited low oral bioavailability (OBAV) and therefore required a pro

219 type-1a and -1b replicons, respectively, and oral bioavailabilities of 38-108% in preclinical species

220 Pharmacokinetic analysis found the oral bioavailability of (125)I-PrP(Sc) to be 33.6%.

221 To increase the low oral bioavailability of 1 (3-5%), prodrug derivatives (3

222 This compound had excellent oral bioavailability of 100% in dogs with an estimated h

223 r, bioactive peptide 25 (Ki = 9 nM) achieved oral bioavailability of 18% in rats, which was commensur

224 entrations of approximately 3 micromol/L, an oral bioavailability of 18%, and a t(1/2) of 8.6 hours w

225 pharmacokinetic half-life, and good absolute oral bioavailability of 20.6%, which supports the value

226 ic solvent CDCl3, and one compound showed an oral bioavailability of 21% in rat.

227 (9) exhibited a superior PK profile with an oral bioavailability of 31% (rats), which is comparable

228 ort a novel peptide (15), which displayed an oral bioavailability of 33% in a rat model, thus validat

229 It has a good pharmacokinetic profile with oral bioavailability of 33%.

230 PK in rats and mice (t 1/2 of 2.6 and 1.6 h, oral bioavailability of 37% and 90%) with anti-inflammat

231 llent pharmacokinetics (PK) profile in rats (oral bioavailability of 39% and t(1/2) of 2.4 h).

232 ontaining a 2',3'-carbonate moiety displayed oral bioavailability of 39%.

233 half-life after intravenous dosing of 4.5 h, oral bioavailability of 77%, and a peak liver concentrat

234 In addition, it has an oral bioavailability of 84% and an oral half-life of 3.8

235 th an ED50 of approximately 1.3 mg/kg and an oral bioavailability of 91.1%.

236 o be used to explain the notable increase in oral bioavailability of a somatostatin analog.

237 The oral bioavailability of ABT-263 in preclinical animal mo

238 The oral bioavailability of AG10, combined with additional d

239 le size fraction for evaluating the relative oral bioavailability of chemicals from soil, which inclu

240 provide a strong basis for establishing that oral bioavailability of cPAHs from soil is less than fro

241 However, the poor oral bioavailability of curcumin poses a significant pha

242 To enhance the water solubility and oral bioavailability of DCK analogues, 12 new mono- and

243 However, poor solubility and low oral bioavailability of DIM-14 limit its translational b

244 This study was carried out to improve the oral bioavailability of DIM-14 via self-emulsifying drug

245 traditionally considered to be important for oral bioavailability of drug-like small molecules, altho

246 eved to play critical roles in the favorable oral bioavailability of hydrophobic drugs.

247 mulsion-based delivery systems that increase oral bioavailability of lipophilic nutraceuticals.

248 These complexes increase the oral bioavailability of melarsoprol making them effectiv

249 -glucosamine prodrugs aimed at improving the oral bioavailability of N-acetyl-(d)-glucosamine as its

250 testinal opioid receptors and the negligible oral bioavailability of naloxone, particularly in a prol

251 This study shows superior oral bioavailability of nano-amorphous powders compared

252 tions have also been reported to improve the oral bioavailability of nucleotide analogs, which usuall

253 Because of the low oral bioavailability of PA 22c, a series of prodrugs was

254 Enhancing the oral bioavailability of peptide drug leads is a major ch

255 n, branched carboxylic acid used to increase oral bioavailability of prodrugs.

256 alized on the antimicrobial property and low oral bioavailability of salicylanilide anthelmintics (cl

257 While the oral bioavailability of small organic compounds is often

258 on the key principles that contribute to the oral bioavailability of successful bRo5 compounds and im

259 he new ProTide strategy was shown to enhance oral bioavailability of the corresponding monoester phos

260 Recent studies on the oral bioavailability of the cyclic heptapeptide sanguina

261 A comparison of rat oral bioavailability of the difluorinated compound to th

262 fected the potency, metabolic stability, and oral bioavailability of the inhibitors, as did the varia

263 The oral bioavailability of the initial lead was below 5%; t

264 effort to improve the aqueous solubility and oral bioavailability of the parent compound.

265 ipophilic character of the alkyl chain), the oral bioavailability of these compounds is low.

266 The absolute oral bioavailability of these compounds was lower than 1

267 Starting from an agonist with poor oral bioavailability, optimization led to potent, select

268 ing tested in human subjects to assess their oral bioavailability, pharmacokinetics and toxicity.

269 ice of selected inhibitors demonstrated high oral bioavailability, plasma half-life, and the potentia

270 ay (28-150 nM), good aqueous solubility, and oral bioavailability profiles in mice.

271 Mean relative oral bioavailability ranged from 6.3% to 20%.

272 Relative oral bioavailability (RBA) of the BaP from soil was esti

273 or PI3K yet improved metabolic stability and oral bioavailability relative to 1.

274 unately, the low aqueous solubility and poor oral bioavailability rendered them undesirable developme

275 pharmacokinetic properties with 63% and 61% oral bioavailability, respectively, in rat.

276 In light of its oral bioavailability, safety toxicology profile in anima

277 dulatory mechanisms, good safety profile and oral bioavailability, statins represent a promising ther

278 Oral bioavailability studies in C57BL/6 mice demonstrate

279 ent, (2) soil fractions historically used in oral bioavailability studies, (3) studies of soil adhere

280 ic CYP3A activity, but the reduced midazolam oral bioavailability suggests that moderate alcohol cons

281 do not apply to peptides, and even the high oral bioavailability that is described for a small numbe

282 Nonetheless, despite their limited oral bioavailability, the more lipophilic trioxolanes ge

283 istinct D(4)-selective agonist with superior oral bioavailability to our first-generation clinical ca

284 In addition, with the goal of enhancing the oral bioavailability, two novel classes of potential gua

285 the N-1 amide position resulted in improved oral bioavailabilities, ultimately leading to clinical c

286 Drugs with poor oral bioavailability usually are administered by hypoder

287 erall favorable pharmacokinetic profile with oral bioavailability values of 62%, 78%, and 18% in rats

288 e metabolites and had significantly enhanced oral bioavailability vs parent drug 1 in a mouse model (

289 sorption rate constant was 1.1 hour(-1), and oral bioavailability was 0.63.

290 However, its oral bioavailability was low.

291 Although, oral bioavailability was maintained when the indole mole

292 of 2 was evaluated in rat and dog, and good oral bioavailability was observed in both species.

293 ely 44-fold (pharmacological) enhancement of oral bioavailability was observed with mucoadhesive devi

294 ration, half-life, area under the curve, and oral bioavailability were not different.

295 favorable pharmacokinetic features and good oral bioavailability were observed during animal studies

296 PTP1B inhibitors, but these inhibitors lack oral bioavailability, which limits their potential for d

297 Furthermore, 35 displayed high (78%) rat oral bioavailability with good oral exposure and plasma

298 Pharmacokinetics in mice showed >90% oral bioavailability with sustained therapeutic serum le

299 pithelial permeability, cellular uptake, and oral bioavailability, with extended blood circulation ti

300 ns to increase resistance to proteolysis and oral bioavailability yielded minihepcidins that, after p