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DRUG CLASS:

Capillary permeability modulator

3ms
New P2 trial • Combination therapy • Metastases
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gemcitabine • albumin-bound paclitaxel • certepetide (LSTA1)
4ms
Enrollment closed • Metastases
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gemcitabine • albumin-bound paclitaxel • certepetide (LSTA1)
5ms
Enrollment change • Metastases
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cisplatin • Imfinzi (durvalumab) • gemcitabine • paclitaxel • certepetide (LSTA1)
6ms
Trial completion date • Trial primary completion date • Metastases
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cisplatin • Imfinzi (durvalumab) • gemcitabine • paclitaxel • docetaxel • certepetide (LSTA1)
6ms
Phase classification • Metastases
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cisplatin • Imfinzi (durvalumab) • gemcitabine • paclitaxel • docetaxel • certepetide (LSTA1)
1year
BOLSTER: A Study of LSTA1 When Added to Standard of Care Versus Standard of Care Alone in Patients With Advanced Solid Tumors (clinicaltrials.gov)
P2a, N=120, Recruiting, Lisata Therapeutics, Inc. | Trial completion date: May 2026 --> Dec 2025 | Trial primary completion date: May 2026 --> Dec 2025
Trial completion date • Trial primary completion date • Metastases
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cisplatin • Imfinzi (durvalumab) • gemcitabine • paclitaxel • docetaxel • certepetide (LSTA1)
1year
A phase Ib/II, open-label, multicenter study to evaluate the safety, efficacy, and pharmacokinetics/pharmacodynamics of αvβ3/5 integrin and neuropilin-1 targeting peptide LSTA1 in patients with metastatic pancreatic ductal adenocarcinoma. (ASCO 2023)
Here we report the safety and efficacy results from a Phase Ib/II, multicenter study of LSTA1 plus (SoC) gemcitabine and locally produced nab-paclitaxel in patients with metastatic pancreatic ductal adenocarcinoma (mPDAC). LSTA1 combined with SoC showed an acceptable safety profile in patients with mPDAC. Compared with historical SoC data, LSTA1 plus SoC numerically improved ORR and PFS. Higher NRP1 expression is associated with better ORR and PFS, suggesting NRP1 may be a potential biomarker of LSTA1 plus chemotherapy for mPDAC treatment.
Clinical • P1/2 data • PK/PD data • Metastases
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NRP1 (Neuropilin 1)
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gemcitabine • albumin-bound paclitaxel • certepetide (LSTA1)
1year
Expression and role of deleted in malignant brain tumor protein 1 in acute respiratory distress syndrome rats induced by sepsis (PubMed, Zhonghua Wei Zhong Bing Ji Jiu Yi Xue)
DMBT1 is a novel early biomarker of ARDS by affecting alveolar epithelial cell, alveolar capillary permeability and inflammatory response.
Preclinical • Journal
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IL6 (Interleukin 6) • IL10 (Interleukin 10)
almost2years
Preclinical assessment of the pharmacokinetics, disposition, and duration of action of the dual alphav-integrin and neuropilin-1 targeting peptide CEND-1 (ESMO 2022)
The duration of the tumor-penetrating effect of CEND-1 was evaluated by assessing tumor accumulation of Evans Blue and Doxorubicin in two different models of hepatocellular carcinoma (HCC): TGFα/c-myc-double transgenic mice and HepG2 xenografted mice. Conclusions These results indicate a favourable in vivo PK profile of CEND-1 after intravenous administration and demonstrate a specific and long-lasting tumour homing and tumor penetrability. Therefore, even single injections of CEND-1 may elicit long-lasting tumor PK improvements for co-administered anti-cancer agents.
PK/PD data • Preclinical
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • NRP1 (Neuropilin 1) • TGFA (Transforming Growth Factor Alpha)
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doxorubicin hydrochloride • certepetide (LSTA1)
2years
iRGD mediated delivery of neoantigens to enable immunotherapy in integrin b5-rich tumors (AACR 2022)
Our recent data shows that KrasLSL-G12D/+ Trp53LSL-R172H/+ Pdx1-Cre (KPC) mice treated with iRGD co-administered with Gemcitabine increased survival compared to drug alone. Our preliminary data showed tumor regression in 70%, and complete response in 42% of the mice treated with iRGD plus OVA1. We are now working on adapting this strategy to pancreatic cancer.
Tumor Mutational Burden • IO biomarker
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KRAS (KRAS proto-oncogene GTPase) • TMB (Tumor Mutational Burden) • CD8 (cluster of differentiation 8) • NRP1 (Neuropilin 1) • PDX1 (Pancreatic And Duodenal Homeobox 1)
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KRAS G12D • TMB-L • KRAS G12
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gemcitabine • certepetide (LSTA1)
over2years
SARS-CoV-2 membrane protein causes the mitochondrial apoptosis and pulmonary edema via targeting BOK. (PubMed, Cell Death Differ)
Overall, M protein activated the BOK-dependent apoptotic pathway and thus exacerbated SARS-CoV-2 associated lung injury in vivo. These findings proposed a proapoptotic role for M protein in SARS-CoV-2 pathogenesis, which may provide potential targets for COVID-19 treatments.
Journal
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BCL2 (B-cell CLL/lymphoma 2)
over2years
Salvage Therapy for Relapsed Malignant Pleural Mesothelioma: A Systematic Review and Network Meta-Analysis. (PubMed, Cancers (Basel))
Patients with malignant pleural mesothelioma (MPM) have very poor prognoses, and pemetrexed plus platinum is the standard first-line therapy...Tremelimumab, vorinostat, nivolumab alone, chemotherapy (CTX), asparagine-glycine-arginine-human tumor necrosis factor plus CTX, and nivolumab plus ipilimumab all produced noticeable PFS benefits compared with placebo. Nivolumab plus ipilimumab had the best PFS ranking (SUCRA: 92.3%). Second-line treatment with nivolumab plus ipilimumab provided the OS and PFS outcomes for patients with relapsed MPM.
Retrospective data • Review • Journal
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TNFA (Tumor Necrosis Factor-Alpha)
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Keytruda (pembrolizumab) • Opdivo (nivolumab) • Yervoy (ipilimumab) • Imjudo (tremelimumab) • pemetrexed • Zolinza (vorinostat) • Arenegyr (NGR-hTNF)
over2years
Arsenic-induced lung inflammation and fibrosis in a rat model: Contribution of the HMGB1/RAGE, PI3K/AKT, and TGF-β1/SMAD pathways. (PubMed, Toxicol Appl Pharmacol)
In conclusion, the current study demonstrates that sub-chronic arsenic exposure triggers the inflammatory response and collagen fiber deposition in rat lung tissue. The potential mechanism may be closely related to activation of the pro-inflammatory-related HMGB1/RAGE pathway and initiation of the PI3K/AKT and TGF-β1/SMAD pathways.
Preclinical • Journal
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SMAD4 (SMAD family member 4) • HMGB1 (High Mobility Group Box 1) • IL18 (Interleukin 18) • TGFB1 (Transforming Growth Factor Beta 1) • MMP9 (Matrix metallopeptidase 9) • IL1B (Interleukin 1, beta) • SMAD2 (SMAD Family Member 2) • SMAD3 (SMAD Family Member 3)
over2years
CENDIFOX: CEND-1 in Combination With Neoadjuvant FOLFIRINOX With or Without Panitumumab (clinicaltrials.gov)
P1b/2a, N=50, Recruiting, Anup Kasi | Not yet recruiting --> Recruiting
Clinical • Enrollment open • Combination therapy
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BRAF (B-raf proto-oncogene)
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5-fluorouracil • Vectibix (panitumumab) • oxaliplatin • irinotecan • leucovorin calcium • certepetide (LSTA1)
almost3years
iRGD-liposomes enhance tumor delivery and therapeutic efficacy of antisense oligonucleotide drugs against primary prostate cancer and bone metastasis. (PubMed, Adv Funct Mater)
Overall, we provide here a delivery system that can significantly increase ASO accumulation and efficacy in solid tumors. These benefits are achieved without significant side effects, providing a way to increase the antitumor efficacy of ASOs.
Clinical • Journal
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AR (Androgen receptor)
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AR expression
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certepetide (LSTA1)
over3years
CEND-1 in Combination With Nabpaclitaxel and Gemcitabine in Metastatic Pancreatic Cancer (clinicaltrials.gov)
P1, N=30, Completed, DrugCendR Inc. | Active, not recruiting --> Completed | Trial completion date: Dec 2020 --> Jun 2020 | Trial primary completion date: Nov 2019 --> Jun 2020
Clinical • Trial completion • Trial completion date • Trial primary completion date • Combination therapy
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CA 19-9 (Cancer antigen 19-9)
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gemcitabine • albumin-bound paclitaxel • certepetide (LSTA1)
over4years
The pleura and the endocrine system. (PubMed, Eur J Intern Med)
It can lead to a rise in the releasing factor for growth hormone (GHRH), human beta chorionic gonadotropin (Beta-hCG), and insulin-like growth factor 2 (IGF2). The consequence of such hormonal imbalance include hypertrophic pulmonary osteoarthropathy, gynecomastia, and refractory hypoglycemia, respectively.
Review • Journal
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ER (Estrogen receptor) • IGF2 (Insulin-like growth factor 2)