I am sure that the importance of the Sareum CHK1 patents will become vital if we get good trial outcome. They have most areas covered. Patented discoveries have much more value than unpatented discoveries, especially on good results. Over the years these patent announcements have not even caused a blip in SP, but that could radially change very soon. GLA
Orange, mine was good Mate, Coffee & Lunch with friends from Uni. Good conversation, We didn't talk about UNI staff, books and nothing about our weekly at Uni. We shares ideas, places to go and experience that We've got in place that We've been before as a holiday. (I'm planing for my Holiday this Summer) with my Crazy Italian Girlfriend... lol
SAR, I believe "the best in class" as TIM mention will bring some positive result if He's prove His compound works very well. Waiting time for us, positive news to be out, update, deal and finally We get our reward here. We started a good week Mate, but 0.30 mark still there to be in the past. Obelix
CCT245737 is the first orally active, clinical development candidate CHK1 inhibitor to be described. The IC50 was 1.4nM against CHK1 enzyme and it exhibited>1,000-fold selectivity against CHK2 and CDK1. CCT245737 potently inhibited cellular CHK1 activity (IC50 30-220nM) and enhanced gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. Mouse oral bioavailability was complete (100%) with extensive tumor exposure.
In conclusion, CCT245737 is a new CHK1 inhibitor clinical development candidate scheduled for a first in man Phase I clinical trial, that will use the novel pS296 CHK1 ELISA to monitor target inhibition.
Oral Inhibitors of Checkpoint Kinase 1 (CHK1) IND-enabling pre-clinical development stage This is a collaborative development programme between the Sareum and the CRT Pioneer Fund. A CTA is planned to be filed early in Q1 2016 with Phase 1 clinical trails starting shortly thereafter. CHK1 is activated in response to DNA damage, which may be a consequence of the cancer itself, or intentionally caused by chemotherapy or radiotherapy. CHK1 inhibitors are anticipated to provide a therapeutic strategy for enhancing the effectiveness of DNA damaging chemotherapeutics currently used in cancer treatment, particularly against solid tumours that are driven by p53 defects. These include colon, ovarian, pancreatic and lung cancers. The pre-clinical candidate is a highly selective and nanomolar potent inhibitor. The compound shows oral bioavailability in three species and has a favourable safety pharmacology profile. Strong potentiation of the efficacy of gemcitabine (Figure 1), GemCarbo and irinotecan is observed with oral dosing of the CHK1 candidate in colon, lung and pancreatic cancer xenograft studies. Single agent efficacy is observed with once daily oral dosing in in vivo models of AML, lymphoma and neuroblastoma (Figure 2). The candidate, and other lead series compounds, modulate cellular and in vivo biomarkers including auto- phosphorylation of Ser296 and phosphorylation of CDK1-Tyr15, plus chemotherapeutic induced H2AX phosphorylation and PARP cleavage for up to 24hrs following a single oral dose. These compounds are “drug like” and show excellent (>500 fold) specificity vs CHK2 and CDK1 kinases.
A few years ago 2013 [I think] posters were highly excited that the Christmas of that year would be transformational for SAR and invites were being offered for the SAR 10p party long term posters will remember ]-- I wonder will that party be in 2016
Oblelix, good thanks mate, I had a good one, trust you did too?
In terms of a deal, I suspect the main reason for proceeding is 'best in class' and I imagine that Sareum, with its current global exposure have a significant amount of third party interest....but why sell off the rights to the drug, particularly when you have such a huge percentage chance of getting through the next phase of development?
30mil payments could well go to a few hundred million of payments in the space of the next few months! Just need the update, trial and a proper result, which is stacked in Sar's favour due to the significant amount of time developing the molecule in close collaboration with the worlds leading charity.
There is zero room for error, a slim chance of failure, a very disable chance of changing the worlds cancer treatments.
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