1 525 mg/day is the recommended dose for oral
enzastaurin.
2 cal studies, and clinical study results with
enzastaurin.
3 e basis of plasma exposures and safety data,
enzastaurin 525 mg once daily is the recommended phase I
4 Enzastaurin -
a novel oral antitumor agent that selectiv
5 Enzastaurin,
a PKCbeta inhibitor, blocked PKCbeta activi
6 rve as a reliable pharmacodynamic marker for
Enzastaurin activity.
7 e II trial tested the efficacy and safety of
enzastaurin added to a standard carboplatin/paclitaxel c
8 nducted to determine the recommended dose of
enzastaurin,
an oral protein kinase C beta (PKCbeta) inh
9 Enzastaurin,
an oral serine/threonine kinase inhibitor,
10 In addition, treatment with
Enzastaurin and AR-A014418 decreased the mRNA levels and
11 Total analytes (
enzastaurin and its metabolites) exposure increased with
12 Treatment with a combination of
Enzastaurin and the GSK3 inhibitor AR-A014418 resulted i
13 mpounds, including bortezomib, lenalidomide,
enzastaurin,
and adaphostin.
14 y and demonstrate that the PKCbeta inhibitor
enzastaurin,
and the clinically available anti-hypertens
15 These results demonstrate that
enzastaurin,
at clinically achievable concentrations, in
16 various advanced cancers and suggested that
enzastaurin can be safely used long term in combination
17 Enzastaurin combined with GSK3 inhibitors demonstrated a
18 Furthermore,
enzastaurin demonstrated additive cytotoxicity in combin
19 Enzastaurin displays pro-apoptotic properties against a
20 Furthermore,
enzastaurin downregulated AKT activity and its downstrea
21 ed the novel, orally available PKC-inhibitor
enzastaurin for its anti-MM activity.
22 e PKCbeta-selective small molecule inhibitor
enzastaurin had a similar effect.
23 These data show that
Enzastaurin has a direct antitumor effect and that Enzas
24 Herein, we show that
Enzastaurin has a direct effect on human tumor cells, in
25 KC) isoforms by the small molecule inhibitor
enzastaurin has shown promising preclinical activity in
26 Our studies therefore show that
enzastaurin has significant antitumor activity in WM bot
27 survival, and angiogenesis are abrogated by
enzastaurin in an in vivo xenograft model of human MM.
28 olerability and survival data, evaluation of
enzastaurin in combination with cytotoxic drugs is warra
29 results directly led to a clinical trial for
Enzastaurin in CTCL in which it was well tolerated and s
30 Further studies of
enzastaurin in DLBCL are warranted.
31 ficacy of the orally available PKC inhibitor
enzastaurin in MM and strongly support its clinical eval
32 A recent phase II study of
enzastaurin in patients with relapsed or refractory diff
33 e II study of a potent inhibitor of PKCbeta,
enzastaurin,
in patients with relapsed or refractory DLB
34 at the protein kinase C (PKC) beta inhibitor
Enzastaurin increases apoptosis in malignant lymphocytes
35 Enzastaurin induced dose-dependent apoptosis at 48 hours
36 Enzastaurin-
induced cell death involved caspase-3-activa
37 ore, accumulated beta-catenin contributes to
enzastaurin-
induced cell death.
38 Enzastaurin inhibited Akt phosphorylation and Akt kinase
39 Consequently,
enzastaurin inhibits proliferation, survival, and migrat
40 Our results show that
enzastaurin is an effective chemopreventive agent in a m
41 Enzastaurin is an oral serine/threonine kinase inhibitor
42 ng synergistic cytotoxicity is observed when
enzastaurin is combined with bortezomib and moderate syn
43 Based on these and previous data,
enzastaurin is currently under clinical investigation in
44 Enzastaurin is emerging as a promising new antitumor tre
45 Enzastaurin is well tolerated up to 700 mg/d.
46 Enzastaurin (
LY317615) was initially developed as an ant
47 arget for colon cancer chemoprevention using
enzastaurin (
LY317615), a PKCbeta-selective inhibitor, i
48 The PKCbeta-selective inhibitor,
Enzastaurin (
LY317615.HCl), suppresses angiogenesis and
49 o PI3K/AKT activation, but it is unknown how
enzastaurin may interfere with signaling through this pa
50 evention and the PKCbeta-selective inhibitor
enzastaurin may represent an effective chemopreventive a
51 Enzastaurin not only inhibits protein kinase Cbeta activ
52 Two deaths, unrelated to
enzastaurin,
occurred.
53 he effects of the PKCbeta-specific inhibitor
enzastaurin on the survival of B cells from mice with lu
54 We have investigated the effects of
enzastaurin on the viability of the cutaneous T-cell lym
55 In addition,
enzastaurin overcame tumor cell growth induced by cocult
56 of chemotherapy (paclitaxel/carboplatin +/-
enzastaurin [
PCE/PC]) followed by maintenance therapy (e
57 n [PCE/PC]) followed by maintenance therapy (
enzastaurin/
placebo).
58 a-catenin decreased the cytotoxic effects of
Enzastaurin plus AR-A014418.
59 We find that
enzastaurin potently reduces azoxymethane-induced colon
60 Sle mice with the PKCbeta-specific inhibitor
enzastaurin prevented the development of lupus.
61 Inhibition of PKCbetaII with
enzastaurin reduced A549 cell proliferation by >60% (48
62 Biochemically,
enzastaurin reduces expression of the PKCbetaII- and bet
63 ulation of Fas and DR5, and PKCbeta shRNA or
enzastaurin reversed this effect.
64 Moreover,
enzastaurin sensitized a variety of human tumor cell lin
65 Enzastaurin specifically inhibits phorbol ester-induced
66 reports, these data support the notion that
Enzastaurin suppresses tumor growth through multiple mec
67 ractory diffuse large B-cell lymphoma showed
enzastaurin to be associated with prolonged freedom from
68 Oral dosing with
Enzastaurin to yield plasma concentrations similar to th
69 hibition of tumor growth was observed in the
enzastaurin-
treated mice (P = .028).
70 Enzastaurin treatment also suppresses GSK3beta phosphory
71 Enzastaurin treatment also suppresses the phosphorylatio
72 ive B cells as well as the in vivo effect of
enzastaurin treatment on the development of lupus in Sle
73 aurin has a direct antitumor effect and that
Enzastaurin treatment suppresses GSK3beta phosphorylatio
74 As in cultured tumor cells,
Enzastaurin treatment suppresses the phosphorylation of
75 Enzastaurin-
treatment decreased cell viability, increase
76 This phase II trial of
enzastaurin was conducted to determine the 6-month progr
77 Enzastaurin was taken orally once daily until disease pr
78 Treatment with
enzastaurin was well-tolerated and associated with prolo
79 certain a means of improving the efficacy of
Enzastaurin,
we investigated complementary signaling pat
80 age, 58 years) received at least one dose of
enzastaurin,
with a median of two cycles (range, one to