ライフサイエンスコーパス: bictegravir

1 inhibitors (DTG, raltegravir, elvitegravir, bictegravir), 2 protease inhibitors (darunavir, atazanav

2 Regarding bictegravir, 2 isolates remained susceptible and 2 had a

3 INSTI-CRR was 2.33% (0.15% dolutegravir/bictegravir, 2.29% raltegravir/elvitegravir) and 1.74% t

4 upport the use of single-tablet coformulated bictegravir (30 mg), emtricitabine (120 mg), and tenofov

5 Participants received bictegravir (30 mg), emtricitabine (120 mg), and tenofov

6 om their current regimen to combination oral bictegravir 50 mg, emtricitabine 200 mg, and tenofovir a

7 andomly assigned (1:1) to receive daily oral bictegravir 50 mg, emtricitabine 200 mg, and tenofovir a

8 B virus co-infection to receive coformulated bictegravir 50 mg, emtricitabine 200 mg, and tenofovir a

9 participants (1:1) to receive co-formulated bictegravir 50 mg, emtricitabine 200 mg, and tenofovir a

10 receive treatment with either co-formulated bictegravir 50 mg, emtricitabine 200 mg, and tenofovir a

11 block size of four), to receive coformulated bictegravir 50 mg, emtricitabine 200 mg, and tenofovir a

12 (1:1) to receive oral fixed-dose combination bictegravir 50 mg, emtricitabine 200 mg, and tenofovir a

13 Group 4 received oral daily bictegravir (50 mg), emtricitabine (200 mg), and tenofov

14 alafenamide (15 mg) once daily, switching to bictegravir (50 mg), emtricitabine (200 mg), and tenofov

15 rly every 2 months or to continue daily oral bictegravir (50 mg), emtricitabine (200 mg), and tenofov

16 1 RNA copies per mL for at least 3 months on bictegravir (50 mg), emtricitabine (200 mg), and tenofov

17 ly tenofovir alafenamide (25 mg, group 1) or bictegravir (75 mg, group 2).

18 Bictegravir, a novel, once-daily, unboosted INSTI, showe

19 Administration of bictegravir, a novel, potent, once-daily INSTI designed

20 study comparing initial HIV-1 treatment with bictegravir-a novel INSTI with a high in-vitro barrier t

21 HIV-1-RNA in the bictegravir and dolutegravir groups were <50 copies per

22 The pharmacokinetics of bictegravir and its association with decay of HIV-1 RNA

23 strand transfer inhibitors (dolutegravir and bictegravir) and tenofovir alafenamide, especially in an

24 is burden, including dosing of dolutegravir, bictegravir, and cabotegravir when used with the rifamyc

25 Primary outcomes were bictegravir area under the curve over the dosing interva

26 e inhibitors (NNRTIs), with dolutegravir and bictegravir associated with more weight gain than elvite

27 se inhibitors (NNRTI), with dolutegravir and bictegravir associated with more weight gain than elvite

28 tion of the advanced INSTIs dolutegravir and bictegravir at near-atomic resolution.

29 Bictegravir (B)/emtricitabine (F)/tenofovir alafenamide

30 The efficacy and safety of bictegravir-based antiretroviral therapy in people with

31 Increased use of a bictegravir-based PEP regimen in 2023 suggests a shift i

32 The number of persons prescribed a bictegravir-based PEP regimen increased from 1,377 (4.1%

33 ty outcomes were evaluated after a switch to bictegravir (BIC) (75-mg) + lenacapavir (LEN) (25- or 50

34 The pharmacokinetics of bictegravir (BIC) and its association with the decay of

35 termined total and unbound concentrations of bictegravir (BIC) in cerebrospinal fluid (CSF) in 15 asy

36 iatric HIV/AIDS Cohort Study who switched to bictegravir (BIC), dolutegravir (DTG), elvitegravir (EVG

37 ter), dolutegravir (DTG), raltegravir (RAL), bictegravir (BIC), or cabotegravir (CAB) at clinically r

38 3 years) were included: 142 received 1HP and bictegravir (BIC)-containing regimens (1HP/BIC group), 4

39 us nanofluidic implant co-delivering TAF and bictegravir (BIC).

40 s with human immunodeficiency virus (HIV) on bictegravir (BIC).

41 This retrospective study evaluated Bictegravir (BIC)/emtricitabine (FTC)/tenofovir alafenam

42 as the clinical HIV-1 INSTIs raltegravir and bictegravir bound to the active site of the deltaretrovi

43 tic concentrations, second-generation InSTIs bictegravir, cabotegravir, and dolutegravir decreased hE

44 etroviral-experienced patients, to 5 INSTIs (bictegravir, cabotegravir, dolutegravir, elvitegravir, a

45 Bictegravir co-formulated with emtricitabine and tenofov

46 e aimed to assess the efficacy and safety of bictegravir coformulated with emtricitabine and tenofovi

47 Protein-unbound bictegravir concentrations in SP, RT, and CVF highly exc

48 HIV-1 RNA in CVF at day 14.The median total bictegravir concentrations in SP, RT, and CVF were 65.5

49 Total and protein-unbound bictegravir concentrations were quantified in BP, SP, CV

50 pivirine showed non-inferior efficacy versus bictegravir, emtricitabine, and tenofovir alafenamide (H

51 ed and 631 enrolled and randomly assigned to bictegravir, emtricitabine, and tenofovir alafenamide (n

52 ned 631 participants to receive coformulated bictegravir, emtricitabine, and tenofovir alafenamide (n

53 ) and islatravir (0.75 mg) and 321 continued bictegravir, emtricitabine, and tenofovir alafenamide (t

54 ants were screened, completed treatment with bictegravir, emtricitabine, and tenofovir alafenamide (u

55 INTERPRETATION: At 48 weeks, coformulated bictegravir, emtricitabine, and tenofovir alafenamide ac

56 These long-term data support the use of bictegravir, emtricitabine, and tenofovir alafenamide as

57 These week 96 data support bictegravir, emtricitabine, and tenofovir alafenamide as

58 These week 96 data support bictegravir, emtricitabine, and tenofovir alafenamide as

59 and islatravir (0.75 mg) was non-inferior to bictegravir, emtricitabine, and tenofovir alafenamide at

60 sed the efficacy, safety and tolerability of bictegravir, emtricitabine, and tenofovir alafenamide co

61 r-term efficacy, safety, and tolerability of bictegravir, emtricitabine, and tenofovir alafenamide co

62 deviation and one who withdrew] assigned to bictegravir, emtricitabine, and tenofovir alafenamide di

63 Because coformulated bictegravir, emtricitabine, and tenofovir alafenamide do

64 ere randomly assigned to treatment (327 with bictegravir, emtricitabine, and tenofovir alafenamide fi

65 ine every 2 months with continued once-daily bictegravir, emtricitabine, and tenofovir alafenamide fo

66 t week 2 to confirm the dose of coformulated bictegravir, emtricitabine, and tenofovir alafenamide fo

67 nodeficiency virus infection (PWH) receiving bictegravir, emtricitabine, and tenofovir alafenamide fu

68 d with one (0.3%) of 319 participants in the bictegravir, emtricitabine, and tenofovir alafenamide gr

69 243 initiated treatment (121 in the receive bictegravir, emtricitabine, and tenofovir alafenamide gr

70 urred in 35 (29%) of 121 participants in the bictegravir, emtricitabine, and tenofovir alafenamide gr

71 ion were reported for no participants in the bictegravir, emtricitabine, and tenofovir alafenamide gr

72 One (1%) of 121 participants in the bictegravir, emtricitabine, and tenofovir alafenamide gr

73 12 (long-acting with oral lead-in group and bictegravir, emtricitabine, and tenofovir alafenamide gr

74 d in 92.4% of patients (n=290 of 314) in the bictegravir, emtricitabine, and tenofovir alafenamide gr

75 HIV-1 RNA less than 50 copies per mL in the bictegravir, emtricitabine, and tenofovir alafenamide gr

76 compared with 23 [7.2%] participants in the bictegravir, emtricitabine, and tenofovir alafenamide gr

77 virine group comapred with 38 (11.9%) in the bictegravir, emtricitabine, and tenofovir alafenamide gr

78 HIV-1 RNA less than 50 copies per mL in the bictegravir, emtricitabine, and tenofovir alafenamide gr

79 iority: 113 (95%) of 119 participants in the bictegravir, emtricitabine, and tenofovir alafenamide gr

80 21), and 75 (63%) of 119 participants in the bictegravir, emtricitabine, and tenofovir alafenamide gr

81 d to assess the efficacy of combination oral bictegravir, emtricitabine, and tenofovir alafenamide in

82 Coformulated bictegravir, emtricitabine, and tenofovir alafenamide is

83 Coformulated bictegravir, emtricitabine, and tenofovir alafenamide is

84 tease inhibitor-based regimen to combination bictegravir, emtricitabine, and tenofovir alafenamide is

85 We aimed to investigate whether bictegravir, emtricitabine, and tenofovir alafenamide is

86 The single-tablet regimen consisting of bictegravir, emtricitabine, and tenofovir alafenamide is

87 100 mg) and islatravir (0.75 mg) or continue bictegravir, emtricitabine, and tenofovir alafenamide or

88 h occurred less frequently in patients given bictegravir, emtricitabine, and tenofovir alafenamide th

89 related to study drug were less common with bictegravir, emtricitabine, and tenofovir alafenamide th

90 We investigated a switch from bictegravir, emtricitabine, and tenofovir alafenamide to

91 6; p=0.78), demonstrating non-inferiority of bictegravir, emtricitabine, and tenofovir alafenamide to

92 group (study 1), and six (2%) of 320 in the bictegravir, emtricitabine, and tenofovir alafenamide ve

93 At week 144, bictegravir, emtricitabine, and tenofovir alafenamide wa

94 nalyses of two phase 3 studies, coformulated bictegravir, emtricitabine, and tenofovir alafenamide wa

95 At week 96, bictegravir, emtricitabine, and tenofovir alafenamide wa

96 Bictegravir, emtricitabine, and tenofovir alafenamide wa

97 The fixed-dose combination of bictegravir, emtricitabine, and tenofovir alafenamide wa

98 , and lamivudine) and 645 in study 2 (327 to bictegravir, emtricitabine, and tenofovir alafenamide, 3

99 omly assigned and treated in study 1 (314 to bictegravir, emtricitabine, and tenofovir alafenamide, a

100 Study 2 randomly assigned (1:1) adults to bictegravir, emtricitabine, and tenofovir alafenamide, o

101 7 with oral lead-in) and 223 (33%) continued bictegravir, emtricitabine, and tenofovir alafenamide.

102 rticipants who received at least one dose of bictegravir, emtricitabine, and tenofovir alafenamide.

103 mly assigned 2:1 to receive twice-daily oral bictegravir-emtricitabine-tenofovir alafenamide (50-200-

104 s evidence to support the use of twice-daily bictegravir-emtricitabine-tenofovir alafenamide in peopl

105 he efficacy, safety, and pharmacokinetics of bictegravir-emtricitabine-tenofovir alafenamide twice-da

106 of the INSIGHT trial (NCT04734652) receiving bictegravir/emtricitabine/TAF (BIC/FTC/TAF 50/200/25mg)

107 ART-naive participants who initiated either bictegravir/emtricitabine/TAF (BIC/FTC/TAF) or dolutegra

108 ce, -0.11%; 95% CI, -0.37% to -0.15%), 7 for bictegravir/emtricitabine/tenofovir alafenamide (0.38% o

109 ne (DTG/3TC, n = 89) or to switch or stay on bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF

110 naive were randomized (2:1) to DTG + 3TC or bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC

111 nd Prevention (CDC) in 2016 and of off-label bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC

112 omparative effectiveness and tolerability of bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC

113 evaluated whether switching from DTG/3TC to bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC

114 bility and 301 were randomly assigned to the bictegravir group (n=153) or to the boosted protease inh

115 Two individuals died in the bictegravir group (recreational drug overdose and suicid

116 due to adverse events (5 [2%] of 320 in the bictegravir group and 1 [<1%] 325 in the dolutegravir gr

117 re reported for 89 (28%) participants in the bictegravir group and 127 (40%) in the dolutegravir grou

118 eved by 269 (84%) of 320 participants in the bictegravir group and 281 (86%) of 325 in the dolutegrav

119 weeks; 283 (88%) of 320 participants in the bictegravir group and 288 (89%) of 325 in the dolutegrav

120 eved in 286 (89%) of 320 participants in the bictegravir group and 302 (93%) of 325 in the dolutegrav

121 Of these, 320 in the bictegravir group and 325 in the dolutegravir group rece

122 327 participants were assigned to the bictegravir group and 330 to the dolutegravir group.

123 re was 0.7% (one of 153 participants) in the bictegravir group and 4.1% (six of 148 participants) in

124 023, we enrolled 122 participants: 80 in the bictegravir group and 42 in the dolutegravir group.

125 olment was 49.5 years (IQR 43.6-56.2) in the bictegravir group and 48.0 (40.5-57.4) years in the boos

126 02 copies per mL (IQR 25 074-392 902) in the bictegravir group and 75 545 copies per mL (21 708-559 4

127 re reported for 64 (20%) participants in the bictegravir group and 92 (28%) in the dolutegravir group

128 continuation in six (2%) participants in the bictegravir group and five (2%) in the dolutegravir grou

129 curred in 36 (45%) of 80 participants in the bictegravir group and in 23 (55%) of 42 participants in

130 isease and congestive cardiac failure in the bictegravir group and one unknown causes, one pulmonary

131 iscontinued because of adverse events in the bictegravir group compared with five (2%) of 315 in the

132 Two participants in the bictegravir group did not receive at least one dose of t

133 At week 24, 63 (96.9%) of 65 in the bictegravir group had HIV-1 RNA loads of less than 50 co

134 lated adverse events were less common in the bictegravir group than in the dolutegravir group (57 [18

135 e, with 276 (88%) of 314 participants in the bictegravir group versus 283 (90%) of 315 participants i

136 36 (11%) participants in the bictegravir group versus 39 (12%) participants in the do

137 lutegravir group; one of these events in the bictegravir group versus four in the dolutegravir group

138 vents were diarrhoea (57 [18%] of 320 in the bictegravir group vs 51 [16%] of 325 in the dolutegravir

139 events were nausea (36 [11%] of 314 for the bictegravir group vs 76 [24%] of 315 for the dolutegravi

140 me was the proportion of participants in the bictegravir group with plasma HIV-1-RNA of less than 50

141 200 mg, and tenofovir alafenamide 25 mg (the bictegravir group) or co-formulated dolutegravir 50 mg,

142 and tenofovir alafenamide 25 mg once daily (bictegravir group) or continued their current regimen (a

143 200 mg, and tenofovir alafenamide 25 mg (the bictegravir group) or dolutegravir 50 mg with co-formula

144 ine-tenofovir alafenamide (50-200-25 mg; the bictegravir group) or twice-daily oral dolutegravir (50

145 ere observed in 11 (14%) participants in the bictegravir group, and three (7%) participants in the do

146 enofovir alafenamide fixed-dose combination [bictegravir group] and 330 with dolutegravir plus emtric

147 Bictegravir had a lower IC50 than the other INSTIs on th

148 Recently, bictegravir has been approved for HIV-1, but no data are

149 At therapeutic concentrations, bictegravir induced substantial hESC death and fetal res

150 Bictegravir is a novel, potent INSTI with a high in-vitr

151 Bictegravir may contribute to inhibit viral replication

152 pants (2:1) to receive oral once-daily 75 mg bictegravir or 50 mg dolutegravir with matching placebo

153 strand transfer inhibitors dolutegravir and bictegravir, particularly when coadministered with tenof

154 One participant taking bictegravir plus emtricitabine and tenofovir alafenamide

155 ported by 55 (85%) of 65 participants in the bictegravir plus emtricitabine and tenofovir alafenamide

156 INTERPRETATION: Bictegravir plus emtricitabine and tenofovir alafenamide

157 ing and giving study drug to 98 (65 received bictegravir plus emtricitabine and tenofovir alafenamide

158 320 participants who received the bictegravir regimen and 325 participants who received th

159 o 3.2), demonstrating non-inferiority of the bictegravir regimen compared with the dolutegravir regim

160 1.0, p=0.12), showing non-inferiority of the bictegravir regimen to the dolutegravir regimen.

161 t 48 weeks, virological suppression with the bictegravir regimen was achieved and was non-inferior to

162 ale, 4% transgender) predominantly receiving bictegravir/TAF/FTC (73%) were enrolled.

163 essed on alternative regimens (lenacapavir + bictegravir/tenofovir alafenamide/emtricitabine and CAB

164 t squares mean (GLSM) ratio for AUC(tau) for bictegravir was 7.6% higher than adults (GLSM ratio 107.

165 se results, we did a phase 2 trial comparing bictegravir with dolutegravir.