Proposed Directors of Tirupati Graphite explain why they have requisitioned an GM. Watch the video here.
So maybe the reason for the delay of half year results could be that they would probably had too mention that they have issues of some kind but too do with supply/manufacture/formulation of 1801 and this would delay the Trials Application as these would have too be complete another few weeks grace might be all they need, still speculation until it’s relayed from them though!
That’s correct timeline’s as per the AGM statement RNS in December 2019!
“These data suggest that in SDC-1802 Sareum has a potent, orally-available, small molecule contributor to the immune-oncology field, which could prove advantageous over the biological approaches that currently dominate. Subject to successful progress and financing, human trials are targeted to start in late-2020.”
https://imgur.com/a/yeBsHAv
SRA737 is the most selective CHK1 against CHK2 (don’t know about Esparas) the other one Prexasertib was in trials at the same time at the Anderson and Lilly’s Chk1 was discontinued!
https://imgur.com/a/F3b7yWO
SDC-1802 is a better more selective molecule you can see that in the Patents and pharmacology profile plus it’s got the poster presentation against other immunotherapy’s and only one in Solid Cancer but the patent has to be resolved for T-ALL as it’s got final rejection but can still be attained imo with more time and work!
Ok Basser that’s good with me, I I’m allowed too not like one out of 3 compounds and disclose why when asked by fellow poster Ahfam why, and I don’t mind being wrong if you tell me why I’m wrong and agree when such happens!
But if posters make wild claims then I’m going to ask for evidence why!
So let me put this into context I post my opinions why I’m not too fond of 1801 with prove of why and the chemical structure with selectivity’s!
But I’m at it and get people who spell check posts and have ulterior motives!
Another poster posts that Sareum has Master Patents so other companys can’t patent catalytic Tyk2’s and when asked to further the conversation say it contravenes Sareum Patents and it’s all there if you can be arsed too look!
Did everyone take up the offer, I would be more concerned with other posters motives!
Only one other person on the site is questioning such!
TLL Pharma US patent for their Tyk2!
US Patent - 16/333994
6 April 2020 - Notice of Allowance
22 July 2020 - Issue Notification
https://imgur.com/a/Pcu0jhV
Great Article!
https://lifescivc.com/2021/03/selective-allosteric-tyk2-inhibitors/
WIP what I was pointing out is one compound is totally different too the other there are no similaritys, if it was similar in any kind (each part that makes up the chemistry) this would be pointed out by the Examiner when he/she proceeded with the search part of the Patent before it was approved!
Any news of 737 is out of Sareums control, usually in the past Sierra would RNS and Sareum would follow and comment, however the ICR is pushing the research for 737 and so glad it’s partnered with them otherwise there would be nothing, no sign as yet from Sierra, but eventually there will be something in the future Esparas Pharma phase 1/2 trials end soon so I think they will watch this data, could be they need extra time too sort out current formulation issues and have no tox in pre clinic higher doses and completion of pre-clinical and CTA!
IP protection you Patent a group of compounds as in the latest patents Sareum had too choose between 2 groups too Patent!
WIP here is the Structure of both!
SDC-1802
2-(2,6-dichloro-phenyl)-5-[4-(morpholine-4-carbonyl)-phenylamino]-oxazole-4-carboxylic acid amide
TLL018
1h-furo[3,2-b]imidazo[4,5-d]pyridine
Like this Patent from TLL Pharma 018, it has a master frame work as you call it and they patent a group of compounds!
https://imgur.com/a/PQNNwKP
This has IC50 of JAK1 = 4nm
So would say it’s Catalytic as it inhibits JAK’s the IC50 of TYK2 is 5nm so a dual TYK2/JAK1 inhibitor!
Thoth different molecules have different chemical make up, there’s no Master Patent encompassing catalytic domain!
It’s a Master as far as Sareum in concerned as that’s what they did too create the latest SDC-1802 molecule by using as you call it the master framework and changing the difluorophenyl to dichlorophenyl group and got better Tyk2 differentiation against other JAK’s
Workinginpharma this is more to do with 1802 as better profile as said earlier in the Lupus study’s and Long term survival study was not performed due too a lack of funds, so not sure, the poster presentation for 1802 (Immunotherapeutic effects of the TYK2 inhibitor SAR-20351 in syngeneic tumour models) is a credible study for 1802 anyhow!
The other reason which is black and white and in the Lupus study’s as 1802 having a superior pharmacokinetic profile compared with 1801 but this is Lupus study’s and 1802 is lead candidate for cancer not Lupus, so the better molecule is in a different indication, so why continue with 1801 in Autoimmune if 1802 is better, probably because I think they could sell 1801 too fund 1802, but again would this be attractive to a licenser knowing you would be getting second best molecule as described in the Lupus Study’s!
https://imgur.com/a/XE0iDiY
For me too change my position on 1801 I think there has to be a commitment from and institutional entity or a industry partner with knowledge and a different set of skills to what Sareum has just too give confidence that it’s not just retail share holders taking this forward!
Will a another company risk it or wait to license into p1 trials maybe if they had the molecule in the position to finish pre-clinical with issues done than a placing too push into trials and get institution behind them then that’s an ideal situation too progress, I want a plan too go forward because looking at the past it’s been very slow looking at the RNS then the co-development agreement with SRI was in April 2013
Sareum and SRI International entered into a co-development agreement to develop TYK2 inhibitors for autoimmune and inflammatory diseases in April 2013 so that’s coming up 8 years now, we need too change it up going forward or we keep stagnating unfortunately!
If we are due a progress report in a month or so than this is something I want to see, is there still no tox on the higher dose of the newer formulation!
It all depends how much of the molecule you are dosing, if you are not dosing a lower level than a competitor then you are not going too get much tox, it’s only at the highest level that the tox can be gauged, as you can see in the profile the IC50 of JAK1 is very similar too the JAK2, there is a low TYK2 compared with the JAK’s so this is classed a TYK2 inhibitor as it is 38 fold and 43 fold over JAK1 and JAK2 so it’s definitely able to dose a good amount of TYK2 no doubt but let’s see if there are tox issues when at a bigger dose as we were still trying too attain the higher dosing!
But too put in perspective
TLL 018 = 200x fold
Nimbus = 148x and 210x fold
BMS is 50kx fold