The company developing ONCT-534 will take part at Oppenheimer 34th Annual Healthcare Life Sciences Conference next week, hopefully we will have some new data about this very promising DAARI molecule
ONCT-534 some trial data soon? - Advanced Prostate...
ONCT-534 some trial data soon?


I always thought of we can inhibit the N terminal domain we would have a powerful tool. This ONCT-534 works on both the NTD and LBD Ligand Binding Domain. This is excellent for androgen spliced variants castrate resistant PC
oncternal.com/pipeline/onct... Mechanism of Action
As a Dual-Action Androgen Receptor Inhibitor or DAARI, ONCT-534 has a potentially novel and unique mechanism of action: it interacts with both ends of the AR, the N terminal domain (NTD) and the LBD, inhibiting AR function and leading to AR protein degradation. We believe that this NTD binding is relevant to the activity of ONCT-534 against tumors expressing AR splice-variants by preventing AR activation. In this respect, ONCT-534 is designed to mechanistically differ from classical non-steroid antiandrogens that interfere with androgen synthesis, such as abiraterone, and to differ from current standard of care treatment options, such as enzalutamide, darolutamide, or apalutamide, that bind only to the LBD of the AR, which may explain their reduced efficacy in patients with AR-SV-expressing tumors, as these AR variants lack most or all of the LBD. We believe that the differentiated dual-action pharmacology of ONCT-534 has the potential to help men with prostate cancer that is resistant to current standard of care treatments by virtue of amplified AR, LBD mutations, or AR splice variants with loss of LBD. Importantly, ONCT-534 is also active in preclinical models of prostate cancer with a normal, unmutated AR.
I have made you happy it seems!!
It’s a much better option for when I/we become castrate resistant than chemo
Hopefully the FDA won’t make us run the chemo gauntlet first
How about this (another drug, maybe you know it already) let's see if you guess: "XXXX is a novel cytotoxic drug candidate that, through its alendronate moiety, targets osteoclasts in bone metastases and inhibits the vicious cycle. The decrease, especially in CTX, reflects its mode of action. Although used in a predetermined limited number of cycles, it proved active at all three doses and in the vast majority of cases. BSI demonstrated decreased bone metastatic burden. XXXX was effective in CRPC treatment-naïve, as well as heavily pretreated patients."