ライフサイエンスコーパス: oral bioavailability

1 e and transparent delivery systems with high oral bioavailability.

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

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

4 studies, including low clearances and decent oral bioavailability.

5 wing to several advantages including greater oral bioavailability.

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

7 dried powders of itraconazole to enhance its oral bioavailability.

8 nimal toxicity against normal cells and good oral bioavailability.

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

10 a disulfide bond with side chains improving oral bioavailability.

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

12 humans to evaluate a possible improvement in oral bioavailability.

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

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

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

16 erparts, severely limiting exposure time and oral bioavailability.

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

18 31 with desirable potency, selectivity, and oral bioavailability.

19 d improved metabolic stability and increased oral bioavailability.

20 lity increase appears linked to the improved oral bioavailability.

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

22 le polymer chosen for its ability to improve oral bioavailability.

23 cy screen to rapidly identify compounds with oral bioavailability.

24 led to meet criteria required for sufficient oral bioavailability.

25 tive at low nanomolar concentrations and has oral bioavailability.

26 es with the highest possibility of achieving oral bioavailability.

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

28 subsequent analogues suffered from a lack of oral bioavailability.

29 the physicochemical space for optimum human oral bioavailability.

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

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

32 ent on the physicochemical space to optimize oral bioavailability.

33 nhibitors with enhanced potency and improved oral bioavailability.

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

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

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

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

38 ich demonstrated the antitumor efficacy with oral bioavailability.

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

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

41 retained factor Xa binding affinity and good oral bioavailability.

42 selective ROCK1 inhibitor but possessed poor oral bioavailability.

43 ity, cell permeability, and in certain cases oral bioavailability.

44 asible and potential strategy to improve the oral bioavailability.

45 the gastrointestinal tract, leading to poor oral bioavailability.

46 T inhibitors are limited by their potency or oral bioavailability.

47 single dose administration showing favorable oral bioavailability.

48 ffold and endowed with better solubility and oral bioavailability.

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

50 anced dissolution rate is vital to guarantee oral bioavailability.

51 needed to identify parameters that influence oral bioavailability.

52 water and lipids and therefore can influence oral bioavailability.

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

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

55 and two carboxylates, severely limiting its oral bioavailability.

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

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

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

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

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

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

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

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

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

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

66 0b, AZD9496), a clinical candidate with high oral bioavailability across preclinical species that is

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

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

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

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

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

72 Since tipifarnib displays high oral bioavailability and acceptable pharmacokinetic prop

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

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

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

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

77 sed at barrier sites, where it acts to limit oral bioavailability and brain penetration of substrates

78 33 has good stability and oral bioavailability and can cross the blood-brain barri

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

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

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

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

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

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

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

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

87 id not induce in vitro resistance, and shows oral bioavailability and in vivo efficacy.

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

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

90 f 4.3 muM in L6 myoblast cells and excellent oral bioavailability and liver exposure in mice.

91 xcellent pharmacokinetics (PK) profile (high oral bioavailability and low clearance) in multiple prec

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

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

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

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

96 able for in vivo applications due to limited oral bioavailability and metabolic stability.

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

98 s containing such a salt bridge reached high oral bioavailability and oral exposure.

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

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

101 They have good oral bioavailability and pharmacokinetics and induced co

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

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

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

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

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

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

108 e most potent modulator D11 that showed good oral bioavailability and significant in vivo therapeutic

109 lective pharmacological TRPC6 inhibitor with oral bioavailability and suitable pharmacokinetics to am

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

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

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

113 harmacophores while retaining solubility and oral bioavailability, and achieving circulating free pla

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

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

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

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

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

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

120 d selectivity, long lung retention time, low oral bioavailability, and proven efficacy in the lipopol

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

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

123 ivity in human polymorphonuclear leukocytes, oral bioavailability, and target engagement in vivo and

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

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

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

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

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

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

130 e arrived at with no toxicity and acceptable oral bioavailability as potential sweetener candidates.

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

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

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

134 netic (PK) parameters, including substantial oral bioavailability, brain penetration, and significant

135 ith desired FXIa inhibitory potency and good oral bioavailability but high in vivo clearance.

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

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

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

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

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

141 hydroxypropyl-beta-cyclodextrin yielded good oral bioavailability, encouraging progression to in vivo

142 an OVCAR-3 xenograft model demonstrated good oral bioavailability, excellent brain penetration, and e

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

144 rovements-including increase of the relative oral bioavailability F(rel) from 3 to >=100%-led to a hi

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

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

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

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

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

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

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

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

153 d pharmacokinetic properties, including good oral bioavailability for most compounds.

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 nly a single double prodrug with very modest oral bioavailability has reached human therapy as a mark

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

160 , has extremely low water solubility and low oral bioavailability; however, despite these problems, v

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

162 Oral bioavailability in dogs indicated that C18-based an

163 r, compound 2 showed high clearance and poor oral bioavailability in its pharmacokinetics studies.

164 , including improved Caco-2 permeability and oral bioavailability in mice, and exhibits antiprolifera

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

166 reduced the viability of TNBC cells and had oral bioavailability in mice.

167 st with favorable pharmacokinetics and 70.8% oral bioavailability in mice.

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

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

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

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

172 Oral bioavailability in preclinical species ranged from

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

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

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

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

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

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

179 (3S,5R)-12 showed oral bioavailability in rats and demonstrated blood pres

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

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

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

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

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

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

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

187 carbamate P1 linker which provided improved oral bioavailability in the imidazole-based 13-membered

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

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

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

191 Insufficient oral bioavailability is considered as a key limitation f

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

193 However, the oral bioavailability is estimated to be only 10%, which

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

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

196 fforts focusing on potency, selectivity, and oral bioavailability led to the discovery of the potent,

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

198 patocellular carcinoma activity but its poor oral bioavailability limits its further development as a

199 Poor oral bioavailability limits the use of curcumin and othe

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

201 Oral bioavailability, low off-target activity, favorable

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

203 and liver microsomes but showed only limited oral bioavailability (<1%) in rats.

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

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

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

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

208 ved and in silico predictions suggested good oral bioavailability, no PAINS similarities, and ADMET r

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

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

211 atible oral insulin formulation shows a high oral bioavailability of >40%, offers the possibility to

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

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

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

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

216 ose (200 mug/kg) of EL-CSG showed a relative oral bioavailability of 19.5%, compared with subcutaneou

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

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

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

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

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

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

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

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

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

226 surface like an antibody while achieving the oral bioavailability of a small molecule.

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

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

229 As the oral bioavailability of acetaminophen in critically ill

230 The oral bioavailability of AG10, combined with additional d

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

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

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

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

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

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

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

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

239 is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs.

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

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

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

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

244 that resulted in a 11.3-fold increase in the oral bioavailability of oxytocin in pigs in the absence

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

246 Effects of dietary P level on the oral bioavailability of Pb present in soil were examined

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

248 g amorphous solid dispersions increasing the oral bioavailability of poorly soluble drugs.

249 eristic of formulations that may enhance the oral bioavailability of poorly soluble drugs.

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

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

252 While the oral bioavailability of small organic compounds is often

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

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

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

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

257 The oral bioavailability of the encapsulated molecules and t

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

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

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

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

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

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

264 These data identified compounds whose oral bioavailability or brain penetration may be affecte

265 P-gp expression may adversely affect the oral bioavailability or brain penetration of these compo

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

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

268 cteria showed that 60% of the compounds have oral bioavailability potential.

269 cetin are anyway challenged by its very poor oral bioavailability profile and any attempt to overcome

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

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

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

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

274 optimization to improve BD2 selectivity and oral bioavailability resulted in the clinical developmen

275 is hampered by very low and highly variable oral bioavailabilities resulting from their poor absorpt

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

281 Genistein) for further examination of their oral bioavailability through molecular properties, drug

282 dified to design leads that have either high oral bioavailability to treat systemic infections or low

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

284 Drugs with poor oral bioavailability usually are administered by hypoder

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

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

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

288 However, its oral bioavailability was low.

289 ass spectrometry-based characterization, its oral bioavailability was measured in the fasted state wi

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

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

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

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

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

295 sors 6a and 6d demonstrated impressive mouse oral bioavailability with 6a, providing effective in viv

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

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

298 showed considerable exposure levels and good oral bioavailability, with detectable distribution to th

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