| To: Jongmans who wrote (441) | 7/11/1999 11:12:00 PM | | From: RCMac | | | |
Finally, SIBI/BMY Alzheimer's collaboration will begin clinical trials by year-end.
Thursday's report about ELN(Athena)'s work toward an Alzheimer's vaccine took all the headlines (lots of chatter on CNBC, lead stories on TV network news, WSJ and other major newspaper articles, etc), but the WSJ article also noted the good news that BMY would begin clinical trials of SIBI's anti-amyloid plaque protease inhibitor drug candidate:
"[I]f initial safety trials go well [BMY] will quickly move into large-scale tests of effectiveness. In a high-risk gambit to get a drug to market faster, the company will simultaneously conduct four large trials . . . rather than the more typical procedure of conducting consecutive rounds of efficacy trials. . . . The trials will involve several thousand patients and last as long as two years." (WSJ 7/8/99, p. A8, continuation of ELN/Alzheimer's article on front page - hardcopy, sorry, I don't access the interactive edition).
BMY will apparently be spending serious money on these trials. Its apparent strong commitment to development hasn't, I believe, been publicized before now. The 4/30/99 SIBI 10-K noted only that the "most advanced compounds from this [BMY Alzheimer's] collaboration are in pre-clinical development" [p. 10, see also table from p.6, included in post #308 on this thread Message 8680842 .
Rick Harmon's post #384 noted that SIBI IR was still saying early this month that SIBI "expected to hear of clinical plans soon" techstocks.com , Rick having earlier muttered a couple of times about how tight-lipped SIBI was being about this collaboration , e.g. techstocks.com )
On the ELN/Athena effort, see also: techstocks.com
--RCM |
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| To: RCMac who wrote (442) | 7/12/1999 2:03:00 AM | | From: scaram(o)uche | | | |
>> In a high-risk gambit to get a drug to market faster, the company will
simultaneously conduct four large trials . . . . <<
Nice. Won't be boring, although it's becoming "believe it when I see it" material. |
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| To: Czechsinthemail who wrote () | 7/17/1999 1:29:00 PM | | From: scaram(o)uche | | | |
J Pharmacol Exp Ther 1999 Jul;290(1):170-81
SIB-1757 and SIB-1893: selective, noncompetitive antagonists of
metabotropic glutamate receptor type 5.
Varney MA, Cosford ND, Jachec C, Rao SP, Sacaan A, Lin FF, Bleicher L, Santori EM, Flor PJ, Allgeier H,
Gasparini F, Kuhn R, Hess SD, Veli elebi G, Johnson EC
SIBIA Neurosciences, Inc., La Jolla, California.
[Medline record in process]
Cell lines expressing the human metabotropic glutamate receptor subtype 5a (hmGluR5a) and hmGluR1b were used as targets
in an automated high-throughput screening (HTS) system that measures changes in intracellular Ca2+ ([Ca2+]i) using
fluorescence detection. This functional screen was used to identify the mGluR5-selective antagonist, SIB-1757
[6-methyl-2-(phenylazo)-3-pyridinol], which inhibited the glutamate-induced [Ca2+]i responses at hmGluR5 with an IC50 of
0.37 &mgr;M compared with an IC50 of >100 &mgr;M at hmGluR1. Schild analysis demonstrated a noncompetitive
mechanism of inhibition. Pharmacophore mapping was used to identify an additional compound, SIB-1893
[(E)-2-methyl-6-(2-phenylethenyl)pyridine], which was also shown to block glutamate-induced increases in [Ca2+]i at
hmGluR5 with an IC50 of 0.29 &mgr;M compared with an IC50 of >100 &mgr;M at hmGluR1. SIB-1757 and SIB-1893
showed little or no activity when tested for agonist and antagonist activity at the other recombinant human mGluR subtypes,
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid, kainate, and N-methyl-D-aspartate receptors. In rat neonatal
brain slices, SIB-1757 and SIB-1893 inhibited (S)-3,5-dihydroxyphenylglycine (DHPG)-evoked inositol phosphate
accumulation in hippocampus and striatum by 60% to 80%, with a potency similar to that observed on recombinant mGluR5.
However, in the cerebellum, a brain region with low mGluR5 expression, SIB-1757 failed to inhibit DHPG-evoked inositol
phosphate accumulation. In cultured rat cortical neurons, SIB-1757 and SIB-1893 largely inhibited DHPG-evoked [Ca2+]i
signals, revealing a population of neurons that were less sensitive to SIB-1757 and SIB-1893. This is the first description of
highly selective, noncompetitive mGluR5 antagonists. These compounds will be useful tools in evaluating the role of mGluR5 in
normal physiology and in animal models of disease. |
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| To: scaram(o)uche who wrote (448) | 7/17/1999 7:26:00 PM | | From: tommysdad | | | |
While wading through the 23 (!!) U.S. patents issued to Sibia in the past year and a half, this one popped up:
patents.uspto.gov
Anyone care to comment on why Sibia has been assigned this patent? Not exactly "neurosciences".
BTW, 23 U.S. patents in a year and a half is unbelievable for a company this size -- more than any other biotech I follow. Very productive group (of both scientists AND attorneys).
TIA |
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