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DRUG:

ETC-159

i
Other names: ETC159, ETC1922159 , ETC 1922159, ETC-159, ETC-1922159
Associations
Company:
A*Star, Experimental Therapeutics Centre, National University of Singapore
Drug class:
PORCN inhibitor
Associations
4ms
ETC-159-02: ETC-159 In Combination With Pembrolizumab In Advanced MSS/pMMR Ovarian Cancers (clinicaltrials.gov)
P1, N=16, Recruiting, National University Hospital, Singapore | Not yet recruiting --> Recruiting
Enrollment open • pMMR
|
Keytruda (pembrolizumab) • Prolia (denosumab) • zoledronic acid • ETC-159
1year
A Study to Evaluate the Safety and Tolerability of ETC-1922159 as a Single Agent and in Combination With Pembrolizumab in Advanced Solid Tumours (clinicaltrials.gov)
P1, N=89, Active, not recruiting, EDDC (Experimental Drug Development Centre), A*STAR Research Entities | Trial completion date: May 2024 --> Oct 2024 | Trial primary completion date: Feb 2024 --> Oct 2024
Trial completion date • Trial primary completion date • Combination therapy • Metastases
|
RSPO2 (R-Spondin 2) • RSPO3 (R-Spondin 3)
|
RSPO3 fusion
|
Keytruda (pembrolizumab) • ETC-159
over1year
New P1 trial • Combination therapy • Metastases
|
Keytruda (pembrolizumab) • Prolia (denosumab) • zoledronic acid • ETC-159
2years
A Study to Evaluate the Safety and Tolerability of ETC-1922159 as a Single Agent and in Combination With Pembrolizumab in Advanced Solid Tumours (clinicaltrials.gov)
P1, N=89, Active, not recruiting, EDDC (Experimental Drug Development Centre), A*STAR Research Entities | Recruiting --> Active, not recruiting | Trial completion date: Aug 2024 --> May 2024 | Trial primary completion date: Dec 2022 --> Feb 2024
Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy • Metastases
|
RSPO2 (R-Spondin 2) • RSPO3 (R-Spondin 3)
|
RSPO3 fusion
|
Keytruda (pembrolizumab) • ETC-159
2years
EFFICACY OF THE PORCUPINE INHIBITOR ETC-1922159 (ETC-159) PLUS PEMBROLIZUMAB IN MICROSATELLITE STABLE (MSS) OR PROFICIENT MISMATCH REPAIR (PMMR) PLATINUM RESISTANT OVARIAN CARCINOMAS (PROC) (IGCS 2023)
Six PROC patients were treated with the combination in dose escalation & expansion. The majority (66%) were high- grade serous ovarian carcinomas with a median 4 lines (2-7) of previous treatments. SAEs were pneumonitis and erythema with fever (8 mg, 1 patient).
Clinical • Mismatch repair • BRCA Biomarker • PARP Biomarker • PD(L)-1 Biomarker • IO biomarker
|
BRCA2 (Breast cancer 2, early onset)
|
BRCA2 mutation
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Keytruda (pembrolizumab) • ETC-159
over2years
ETC-159, an Upstream Wnt inhibitor, Induces Tumour Necrosis via Modulation of Angiogenesis in Osteosarcoma. (PubMed, Int J Mol Sci)
Consistent with our hypothesis, we noted that ETC-159 treatment not only resulted in markedly decreased β-catenin staining in xenografts, but also increased tumour necrosis and a significant reduction in vascularity-a hereby yet undescribed phenotype following ETC-159 treatment. Through further understanding the mechanism of this new window of vulnerability, therapies can be developed to potentiate and maximize the effectiveness of ETC-159, further increasing its clinical utility for the treatment of OS.
Journal
|
CTNNB1 (Catenin (cadherin-associated protein), beta 1)
|
ETC-159
over3years
Autocrine canonical Wnt signaling primes noncanonical signaling through ROR1 in metastatic castration-resistant prostate cancer. (PubMed, Cancer Res)
IHC confirmed tumor cell WLS expression in primary prostate cancer and mCRPC, and patient-derived prostate cancer xenografts expressing WLS were responsive to treatment with Wnt synthesis inhibitor ETC-1922159...These findings reveal that Wnt/β-catenin signaling in PC drives stem cell maintenance and invasion and primes for noncanonical Wnt signaling through ROR1. They further show that autocrine Wnt production is a nongenomic driver of canonical and noncanonical Wnt signaling in PC, which can be targeted with Wnt synthesis inhibitors to suppress tumor growth.
Journal
|
RUNX1 (RUNX Family Transcription Factor 1) • ROR1 (Receptor Tyrosine Kinase Like Orphan Receptor 1)
|
ETC-159
almost4years
A Study to Evaluate the Safety and Tolerability of ETC-1922159 as a Single Agent and in Combination With Pembrolizumab in Advanced Solid Tumours (clinicaltrials.gov)
P1, N=89, Recruiting, EDDC (Experimental Drug Development Centre), A*STAR Research Entities | Trial completion date: Apr 2023 --> Aug 2024
Clinical • Trial completion date • Combination therapy
|
RSPO2 (R-Spondin 2) • RSPO3 (R-Spondin 3)
|
Keytruda (pembrolizumab) • ETC-159
over4years
A Study to Evaluate the Safety and Tolerability of ETC-1922159 as a Single Agent and in Combination With Pembrolizumab in Advanced Solid Tumours (clinicaltrials.gov)
P1, N=83, Recruiting, EDDC (Experimental Drug Development Centre), A*STAR Research Entities | Trial completion date: Jul 2023 --> Apr 2023
Clinical • Trial completion date • Combination therapy
|
RSPO2 (R-Spondin 2) • RSPO3 (R-Spondin 3)
|
Keytruda (pembrolizumab) • ETC-159
5years
[VIRTUAL] Development of a qRT-PCR-based diagnostic test to identify colorectal cancer patients with recurrent R:Spondin gene fusions (ESMO Asia 2020)
This CTA is currently used to pre-screen & select patients for the phase IB trial with the porcupine inhibitor ETC-1922159 (NCT02521844) ongoing in Singapore and USA...Funding: BMRC, NRF and NMRC Singapore. Clinical trial identification: NCT02521844.
Clinical
|
KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
|
KRAS mutation • BRAF mutation • NRAS mutation
|
Archer® FusionPlex® Oncology Research Kit
|
ETC-159
5years
[VIRTUAL] Development of a qRTPCRbased diagnostic test to identify colorectal cancer patients with recurrent RSpondin gene fusions (ESMO Asia 2020)
This CTA is currently used to pre-screen & select patients for the phase IB trial with the porcupine inhibitor ETC-1922159 (NCT02521844) ongoing in Singapore and USA. BMRC, NRF and NMRC Singapore.
Clinical
|
KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
|
KRAS mutation • BRAF mutation • NRAS mutation
|
ETC-159
5years
[VIRTUAL] Development of a qRTPCRbased diagnostic test to identify colorectal cancer patients with recurrent RSpondin gene fusions (ESMO Asia 2020)
This CTA is currently used to pre-screen & select patients for the phase IB trial with the porcupine inhibitor ETC-1922159 (NCT02521844) ongoing in Singapore and USA. BMRC, NRF and NMRC Singapore.
Clinical
|
KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
|
KRAS mutation • BRAF mutation • NRAS mutation
|
ETC-159