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- ONC206 / Oncoceutics, ONC201 / Oncoceutics
[VIRTUAL] Molecular differentiation of imipridones ONC201 and ONC206 () - Oct 24, 2020 - Abstract #SNO2020SNO_783;
In summary, ONC206 exhibits increased non-competitive DRD2 antagonism, nanomolar potency, distinct biodistribution, differentiated gene expression and disruption of DRD2 dimers relative to ONC201. Thus, ONC206 may be uniquely poised to address tumors that are not addressed by ONC201 or have developed acquired resistance.
- azacitidine / Generic mfg.
[VIRTUAL] International preclinical drug discovery and biomarker program informing an adoptive combinatorial trial for diffuse midline gliomas () - Oct 24, 2020 - Abstract #SNO2020SNO_728;
In vitro (n=15) and in vivo (n=8) models of DMGs across ten institutions were used to assess single and combination treatments with ONC201, ONC206, marizomib, panobinostat, 5-Azacytidine, Val-083, GDC0084 and TAK228. Thorough preclinical testing in a multi-site laboratory setting is feasible and identified ONC201 in combination with ONC206, TAK228 and GDC0084 as promising therapeutics for DMGs.
- ONC206 / Oncoceutics
[VIRTUAL] Biomarker evaluation for imipridone ONC206 reveals ClpP, ATF4, MYC, EGFR and HIF1 as key predictors of anti-cancer efficacy () - Oct 24, 2020 - Abstract #SNO2020SNO_469;
Ongoing studies are further investigating tumor type enrichment of biomarkers. Prediction of innate imipridone sensitivity using biomarkers identified in this study may guide patient and tumor type selection in clinical trials.
- [VIRTUAL] Activation of the Mitochondrial ClpP protease is Synthetically Lethal with HDAC1/2 Inhibition in Glioblastoma Model Systems () - Oct 24, 2020 - Abstract #SNO2020SNO_424;
Finally, using a PDX model, we demonstrated that the combination treatment of romidepsin and ONC206 reduced tumor growth more potently than single treatments or vehicle by enhanced reduction of cellular proliferation and pronounced induction of cell death in vivo. Collectively, these observations suggest that the efficacy of HDAC-inhibitors might be significantly enhanced through ClpP activators in model systems of human GBM.
- ONC206 / Oncoceutics
[VIRTUAL] IND-enabling characterization of dual DRD2- and ClpP-targeting agent ONC206 as the next imipridone for clinical neuro-oncology () - Oct 24, 2020 - Abstract #SNO2020SNO_77;
The no-observed-adverse-effect level was ≥ 16.7 mg/kg in dogs and ≥ 50 mg/kg in rats that exceed efficacious doses. A 50 mg starting dose of ONC206 was selected for the first-in-human open label, dose escalation, and food effect Phase I study in biomarker-enriched adult recurrent primary CNS tumors.
- ||| ONC206 / Chimerix
Enrollment open: Phase I Study of Oral ONC206 in Recurrent and Rare Primary Central Nervous System Neoplasms (clinicaltrials.gov) - Oct 1, 2020
P1, N=102, Recruiting, Sponsor: Oncoceutics, Inc.
A 50 mg starting dose of ONC206 was selected for the first-in-human open label, dose escalation, and food effect Phase I study in biomarker-enriched adult recurrent primary CNS tumors. Not yet recruiting --> Recruiting
- ||| ONC206 / Chimerix
New P1 trial: Phase I Study of Oral ONC206 in Recurrent and Rare Primary Central Nervous System Neoplasms (clinicaltrials.gov) - Sep 8, 2020
P1, N=102, Recruiting, Sponsor: Oncoceutics, Inc.
- | paclitaxel / Generic mfg.
Journal: Targeting Dopamine Receptor D2 by Imipridone Suppresses Uterine Serous Cancer Malignant Phenotype. (Pubmed Central) - Sep 2, 2020
This study provides the first evidence that ONC206 induced metabolic reprogramming in USC cells and is a promising therapeutic agent for USC treatment. These findings support further development of ONC206 as a promising therapeutic agent and improves survival rates in patients with USC.
- ||||| ONC206 / Oncoceutics
Preclinical: Tx options are limited for most recurrent & rare primary CNS cancers. #ONC206 is a next gen imipridone w complete antagonism/ specificity for DRD2. ONC206 showed broad spectrum anti-cancer efficacy in vitro across many solid tumors, esp neuro tumors. It is well-tol. (Twitter) - May 30, 2020
- |||| ONC206 / Oncoceutics, ONC201 / Oncoceutics
👀Trial watch: ph I: oral ONC206 in recurrent & rare #CNS neoplasms. led by my friend Dr Theeler & @NIHBrainTumor team! Blockade of DRD2 has emerged as a target in neuro-onc. #ONC201, a 1st-gen imipridone antagonizes DRD2 & has activity in #H3K27M-mut gliomas #asco20 #btsm (Twitter) - May 30, 2020
- ONC206 / Oncoceutics
IND-enabling characterization of ONC206 as the next bitopic antagonist for oncology (Virtual Meeting II: All Session Times Are U.S. EDT) - May 16, 2020 - Abstract #AACRII2020AACR-II_4904;
A 50 mg starting dose of ONC206 was selected for the first-in-human clinical trial in biomarker-enriched adult recurrent CNS tumors. In summary, ONC206 is poised for clinical Introduction as the next imipridone bitopic DRD2 antagonist for oncology that exhibits differentiated target engagement, signaling, and biodistribution profiles.
- ONC206 / Oncoceutics, Lynparza (olaparib) / Merck (MSD), AstraZeneca
Olaparib potentiates the anti-proliferative and anti-metastatic effects of ONC206 in ovarian cancer cells (Virtual Meeting II: E-Posters) - May 16, 2020 - Abstract #AACRII2020AACR-II_4034;
The imipridone ONC206, a chemical derivative of ONC201, is a bioavailable dopamine receptor D2 (DRD2) antagonist that has anti-tumorigenic effects via induction of apoptosis and activation of the integrated stress response. ONC206 in combination with olaparib resulted in synergistic anti-tumorigenic and anti-metastatic effects in OC cell lines, suggesting that this novel dual therapy may be worthy of further exploration in clinical trials in OC.
- paclitaxel / Generic mfg., ONC206 / Oncoceutics
Novel imipridone ONC206 inhibits cell proliferation and induces apoptosis in uterine serous cancer through altering MAPK/AKT signaling network and metabolic reprogramming (Virtual Meeting II: E-Posters) - May 16, 2020 - Abstract #AACRII2020AACR-II_4025;
ONC206 also showed a synergistic effect with paclitaxel in vitro. Further studies which demonstrate the optimal dosage and the efficacy of treatment of USC using ONC206 are warranted.
- ONC206 / Oncoceutics, Lynparza (olaparib) / Merck (MSD), AstraZeneca
A novel dopamine receptor D2 antagonist (ONC206) potentiates the effects of olaparib in endometrial cancer cells through inhibition of cell proliferation and modulation of the mTOR pathway (Virtual Meeting II: E-Posters) - May 16, 2020 - Abstract #AACRII2020AACR-II_4022;
The imipridone ONC206, a chemical derivative of ONC201, is an orally bioavailable dopamine receptor D2 (DRD2) antagonist that has anti-tumorigenic effects in EC via induction of apoptosis and activation of the integrated stress response. Olaparib and ONC206 had synergistic anti-proliferative effects in human endometrioid EC cell lines, suggesting that this novel dual therapy may be worthy of further exploration in clinical trials in EC.
- ONC206 / Oncoceutics, ONC201 / Oncoceutics
Anti-cancer effects of novel imipridone DRD2 antagonists in a panel of human cancer cell lines (Virtual Meeting II: E-Posters) - May 16, 2020 - Abstract #AACRII2020AACR-II_2857;
Our data show potent anti-stem cell maintenance as well as anti-proliferative, anti-migratory, anti-viability and pro-apoptotic activity of both ONC201 and ONC206 on cancer cell lines, with ONC206 showing greater potency than ONC201. Our future directions include utilizing a combinatorial multi-modality therapy to treat a panel of pediatric and adult neurological tumors with ONC 201/206 and other selective inhibitors of tumorigenic pathways to completely eliminate the highly resistant sub-population of cancer stem cells, and delay malignant recurrence.
- [VIRTUAL] Novel imipridone combination therapies targeting oncohistone H3K27M mutant diffuse midline glioma (DMG) (Virtual Meeting II: E-Posters) - May 16, 2020 - Abstract #AACRII2020AACR-II_2545;
Additional combination testing and synergy analysis is ongoing and will be presented. Our findings suggest that H3K27M DMG cells demonstrate increased sensitivity to imipridones ONC206 and ONC212 as single agents and combinational strategies with HDAC inhibitors and etoposide, and provide insights into novel therapies for further clinical testing.
- ONC206 / Oncoceutics
ONC206, an imipridone derivative, induces cell death through activation of the integrated stress response in serous endometrial cancer in vitro (Virtual Meeting II: E-Posters) - May 16, 2020 - Abstract #AACRII2020AACR-II_2375;
Specifically, ONC206 utilizes ISR activation as a significant pathway in the propagation of its anti-proliferative and anti-metastatic effects. Thus, ONC206 may be a promising agent in serous EC which has limited treatment options.
- ONC206 / Oncoceutics
Highly potent dopamine receptor D2 antagonist ONC206 demonstrates anti-tumorigenic activity in endometrial cancer (Metro Toronto Convention Centre - Hall E) - Mar 19, 2020 - Abstract #SGO2020SGO_2577;
ONC206 exhibited nanomolar potency for inhibiting EC cell growth and was efficacious in reducing EC tumor growth in both obese and lean mice. Thus, ONC206 may be a promising therapeutic agent to be explored in future clinical trials in endometrioid EC.
- ONC206 / Oncoceutics
ONC206, a dopamine receptor D2 antagonist, has anti-tumorigenic effects in high-grade serous ovarian cancer (Metro Toronto Convention Centre - Hall E) - Mar 19, 2020 - Abstract #SGO2020SGO_2299;
ONC206 exhibited nanomolar potency for inhibiting OC cell growth and was efficacious in reducing OC tumor growth in both obese and lean mice. Thus, ONC206 may be a promising therapeutic agent to be explored in future clinical trials in HGSOC.
- ONC206 / Oncoceutics
Highly potent dopamine receptor D2 antagonist ONC206 demonstrates anti-tumorigenic activity in endometrial cancer (Metro Toronto Convention Centre - Hall E) - Mar 19, 2020 - Abstract #SGO2020SGO_1945;
ONC206 exhibited nanomolar potency for inhibiting EC cell growth and was efficacious in reducing EC tumor growth in both obese and lean mice. Thus, ONC206 may be a promising therapeutic agent to be explored in future clinical trials in endometrioid EC.
- ONC206 / Oncoceutics
ONC206, a dopamine receptor D2 antagonist, has anti-tumorigenic effects in high-grade serous ovarian cancer (Metro Toronto Convention Centre - Hall E) - Mar 19, 2020 - Abstract #SGO2020SGO_1667;
ONC206 exhibited nanomolar potency for inhibiting OC cell growth and was efficacious in reducing OC tumor growth in both obese and lean mice. Thus, ONC206 may be a promising therapeutic agent to be explored in future clinical trials in HGSOC.
- ONC206 / Oncoceutics
Highly potent dopamine receptor D2 antagonist ONC206 demonstrates anti-tumorigenic activity in endometrial cancer (Metro Toronto Convention Centre - Hall E) - Mar 19, 2020 - Abstract #SGO2020SGO_1288;
ONC206 exhibited nanomolar potency for inhibiting EC cell growth and was efficacious in reducing EC tumor growth in both obese and lean mice. Thus, ONC206 may be a promising therapeutic agent to be explored in future clinical trials in endometrioid EC.
- ONC206 / Oncoceutics
ONC206, a dopamine receptor D2 antagonist, has anti-tumorigenic effects in high-grade serous ovarian cancer (Metro Toronto Convention Centre - Hall E) - Mar 19, 2020 - Abstract #SGO2020SGO_1010;
ONC206 exhibited nanomolar potency for inhibiting OC cell growth and was efficacious in reducing OC tumor growth in both obese and lean mice. Thus, ONC206 may be a promising therapeutic agent to be explored in future clinical trials in HGSOC.
- ONC206 / Oncoceutics
Highly potent dopamine receptor D2 antagonist ONC206 demonstrates anti-tumorigenic activity in endometrial cancer (Metro Toronto Convention Centre - Hall E) - Mar 19, 2020 - Abstract #SGO2020SGO_653;
ONC206 exhibited nanomolar potency for inhibiting EC cell growth and was efficacious in reducing EC tumor growth in both obese and lean mice. Thus, ONC206 may be a promising therapeutic agent to be explored in future clinical trials in endometrioid EC.
- ONC206 / Oncoceutics
ONC206, a dopamine receptor D2 antagonist, has anti-tumorigenic effects in high-grade serous ovarian cancer (Metro Toronto Convention Centre - Hall E) - Mar 19, 2020 - Abstract #SGO2020SGO_375;
ONC206 exhibited nanomolar potency for inhibiting OC cell growth and was efficacious in reducing OC tumor growth in both obese and lean mice. Thus, ONC206 may be a promising therapeutic agent to be explored in future clinical trials in HGSOC.
- ONC206 / Oncoceutics
[VIRTUAL] A first-in-human phase I single-agent dose-escalation, food effect and dose expansion study of oral ONC206 in recurrent and rare primary central nervous system neoplasms. (Poster Board 67) - Feb 27, 2020 - Abstract #ASCO2020ASCO_235;
Exploratory analysis of DRD2 and DRD5 expression, DRD2 dimerization, expression of MYC and N-MYC in tumor tissue in relation to clinical outcomes will also be performed. Research Funding: Oncoceutics
- |||| ONC206 / Oncoceutics
Clinical: Stopped by to see great progress presented by @vvpeaceful on IND-enabling studies with ONC206 as it heads towards clinical trials #SNO2019 (Twitter) - Nov 23, 2019
- | ONC206 / Oncoceutics
Journal: Metabolic Reprogramming by Dual AKT/ERK Inhibition Through Imipridones Elicits Unique Vulnerabilities in Glioblastoma. (Pubmed Central) - Nov 21, 2019
Research Funding: Oncoceutics These results suggest that c-myc expression predicts therapeutic responses to imipridones and that imipridones lead to suppression of tumor cell energy metabolism, eliciting unique metabolic vulnerabilities that can be exploited for clinical relevant drug combination therapies.
- ONC206 / Oncoceutics
IND-enabling characterization of ONC206 as the next bitopic DRD2 antagonist for neuro-oncology (Ballroom Lawn) - Oct 29, 2019 - Abstract #SNO2019SNO_1079;
The highest non-severely toxic dose (HNSTD) was ≥ 16.7 mg/kg in dogs and ≥ 50 mg/kg in rats that exceeds efficacious doses in preclinical models. Using standard allometric scaling, a 90 mg starting dose of ONC206 was selected for the first-in-human clinical trial in biomarker-defined adult recurrent CNS tumors.
- ONC206 / Oncoceutics
Role of ONC-206 in regulating Medulloblastoma tumor progression (Ballroom Lawn) - Oct 29, 2019 - Abstract #SNO2019SNO_609;
Current studies are focusing on exploring the mechanism by which ONC-206 affects MB growth and metastasis. Dissecting this mechanism will be pivotal in predicting the role of this small molecule as a pre-clinical therapeutic for MB treatment.
- ONC206 / Oncoceutics
Imipridone structure activity relationship uncovers ONC206 as the next bitopic DRD2 antagonist for oncology with differentiated receptor pharmacology (Ballroom Lawn) - Oct 29, 2019 - Abstract #SNO2019SNO_409;
Structural mapping revealed that some ONC206-critical allosteric residue interactions are located at the interface of TM-IV and –V that mediates the DRD2 homodimer interface. Thus, ONC206 is a bitopic DRD2 antagonist that may be poised to address oncogenic DRD2 monomers or dimers.
- ONC206 / Oncoceutics
Novel imipridone ONC206 inhibits cell proliferation and induces apoptosis in uterine serous cancer through altering MAPK/AKT/AMPK signaling network and metabolic reprogramming (Board 55: Level 2 - Hall D) - Sep 18, 2019 - Abstract #AACRNCIEORTC2019AACR_NCI_EORTC_487;
These data suggest that ONC206 suppresses USC progression through inhibiting MAPK/AKT network, which subsequently leads to cell cycle arrest, metabolic reprogramming and increased apoptosis. Further studies which demonstrate the optimal dosage and the efficacy of treatment of USC using ONC206 are warranted.