^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG:

PTX-100

i
Other names: PTX-100, PTX 100, GGTI 2418, GGTI2418, GGTI-2418, PTX100
Associations
Trials
Company:
Kirax, Prescient Therap
Drug class:
GGTase I inhibitor
Associations
Trials
25d
Targeted inhibition of FBXL2 confers susceptibility of HER2-negative breast cancer to trastuzumab deruxtecan. (PubMed, Nat Cancer)
Strikingly, GGTi-2418@LNP or ketoconazole@LNP combined with T-DXd induced robust and durable tumor regression in HER2-IHC 0 TNBC xenograft models in female mice. Together, this study highlights that targeted inhibition of FBXL2 combined with T-DXd may be a viable therapeutic strategy for treating HER2-IHC 0 solid tumors.
Journal
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 negative • HER-2 expression • HER-2 elevation
|
Enhertu (fam-trastuzumab deruxtecan-nxki) • PTX-100
6ms
PTX-100-PD-012017: Phase 1 Study of PTX-100 in Patients With Advanced Malignancies With PTCL Expansion Cohort (clinicaltrials.gov)
P1, N=25, Completed, Prescient Therapeutics, Ltd. | Active, not recruiting --> Completed
Trial completion
|
PTX-100
11ms
PTX-100-PD-012017: Phase 1 Study of PTX-100 in Patients With Advanced Malignancies With PTCL Expansion Cohort (clinicaltrials.gov)
P1, N=25, Active, not recruiting, Prescient Therapeutics, Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Apr 2023 --> Jul 2025 | Trial primary completion date: Apr 2023 --> Jul 2025
Enrollment closed • Trial completion date • Trial primary completion date
|
PTX-100
11ms
A Phase 2 Study of PTX 100 in Patients With Relapsed/Refractory CTCL (clinicaltrials.gov)
P2, N=115, Recruiting, Prescient Therapeutics, Ltd. | Not yet recruiting --> Recruiting
Enrollment open
|
PTX-100
12ms
A Phase 2 Study of PTX 100 in Patients with Relapsed/refractory CTCL (clinicaltrials.gov)
P2, N=115, Not yet recruiting, Prescient Therapeutics, Ltd.
New P2 trial
|
PTX-100
over1year
Targeting the RAS upstream and downstream signaling pathway for Cancer treatment. (PubMed, Eur J Pharmacol)
For instance, RTK inhibitors such as imatinib and afatinib selectively target these receptors, hindering ligand binding and reducing signaling initiation...Other inhibitors, like lonafarnib targeting Farnesyltransferase and GGTI 2418 targeting geranylgeranyl Transferase, disrupt post-translational modifications of proteins...Targeting downstream components with RAF inhibitors such as vemurafenib, dabrafenib, and sorafenib, along with MEK inhibitors like trametinib and binimetinib, has shown promising outcomes in treating cancers with BRAF-V600E mutations, including myeloma, colorectal, and thyroid cancers. Furthermore, inhibitors of PI3K (e.g., apitolisib, copanlisib), AKT (e.g., ipatasertib, perifosine), and mTOR (e.g., sirolimus, temsirolimus) exhibit promising efficacy against various cancers such as Invasive Breast Cancer, Lymphoma, Neoplasms, and hematological malignancies. This review offers an overview of small molecule inhibitors targeting specific proteins within the RAS upstream and downstream signaling pathways in cancer.
Review • Journal
|
BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
|
Mekinist (trametinib) • Gilotrif (afatinib) • Zelboraf (vemurafenib) • Tafinlar (dabrafenib) • sorafenib • imatinib • Mektovi (binimetinib) • temsirolimus • Aliqopa (copanlisib) • ipatasertib (RG7440) • sirolimus • apitolisib (GDC-0980) • perifosine (D21266) • PTX-100
over2years
Phase 1 Pharmacodynamic and Pharmacokinetic Study of the Geranylgeranyltransferase I Inhibitor PTX-100 (GGTI-2418) in Patients with Advanced Malignancies (ASH 2023)
Preliminary data from this phase 1 dose escalation study of PTX-100 indicates promising safety profile in this difficult to treat pt population. PTX-100 demonstrated clinical activity in TCL with an ORR of 40%, and a median PFS for all TCL pts of 5.3 months. PD studies demonstrated that the GGT-1 target was engaged with sustained inhibition of RAP1 GG.
Clinical • P1 data • PK/PD data • Metastases
|
KRAS (KRAS proto-oncogene GTPase) • NRAS (Neuroblastoma RAS viral oncogene homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog) • RHOA (Ras homolog family member A) • RAP1A (RAP1A, Member Of RAS Oncogene Family)
|
KRAS mutation • NRAS mutation • HRAS mutation
|
PTX-100
almost6years
Maackia amurensis agglutinin induces apoptosis in cultured drug resistant human non-small cell lung cancer cells. (PubMed, Glycoconj J)
Two Paclitaxel-resistant NSCLC sub-lines (A549/PTX100 and NCI-H460/PTX100) were developed from A549 & NCI-H460 cell lines respectively. MAA interacted with the cell-surface protein(s) of apparent M ~66 kDa and induced apoptosis in both the sub-lines through intrinsic/mitochondrial pathway, involving reduction in mitochondrial trans-membrane potential, up-regulation of Bax, unaltered/decreased expression of Bcl-X, release of mitochondrial cytochrome c into the cytosol and activation of pro-caspases (-9&-3). Our findings highlighted the potential of this plant agglutinin to serve as an apoptosis inducing agent in drug resistant NSCLC cells.
Preclinical • Journal
|
BCL2L1 (BCL2-like 1) • BAX (BCL2-associated X protein)
|
paclitaxel • PTX-100