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DRUG CLASS:

Cytochrome P450 inhibitor

4d
New trial
9d
DRG Explant Model for Understanding Mechanism of Oxaliplatin-Induced Peripheral Neuropathy and Identifying Potential Therapeutic Targets. (PubMed, Antioxidants (Basel))
Oxaliplatin-triggered chemotherapy-induced peripheral neuropathy (CIPN) is a common and debilitating side effect of cancer treatment that limits the efficacy of chemotherapy and negatively impacts patients' quality of life dramatically. Notably, inhibition of TXNIP with verapamil reduced oxidative stress levels. Our results demonstrated the use of DRG explants as an efficient model to study the mechanisms of CIPN and screen for potential treatments.
Journal
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TXNIP (Thioredoxin Interacting Protein)
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oxaliplatin
10d
Enrollment change
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Keytruda (pembrolizumab) • carboplatin • doxorubicin hydrochloride • AiRuiKa (camrelizumab) • albumin-bound paclitaxel • cyclophosphamide • epirubicin • Noxafil (posaconazole)
16d
Potency-enhancing mutations in E3-19K and i-leader increase the cytolytic activity of the PH20/SPAM1-armed oncolytic adenovirus Ad5Δ24RGD. (PubMed, Mol Ther Oncol)
In some cell lines, the fiber modification F5RGD10(2C) or verapamil treatment further improves actual spread efficiency. Nelfinavir inhibits spread and plaque formation of oncolytic adenoviruses with the 19KSS-iLQ125Ter modifications, irrespective of adenovirus death protein (ADP) expression...We identified an insertion site downstream of the L3-23K region that supports relatively high hPH20 activity while preserving the enhanced oncolytic potency of the virus. Combining 19KSS-iLQ125Ter with hPH20 expression may potentially improve therapeutic benefit in glioma.
Journal
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SPAM1 (Sperm Adhesion Molecule 1)
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Viracept (nelfinavir)
16d
Posaconazole attenuates arsenic trioxide toxicity and enhances safety and efficacy while reducing invasion and metastasis in non-small-cell lung cancer. (PubMed, Pulm Pharmacol Ther)
Furthermore, flow cytometry and colony formation assays revealed that PCZ attenuates and reduces the apoptotic/necrotic effects of ATO. In conclusion, PCZ synergistically and effectively reduces the adverse cytotoxic effects of ATO in lung cancer cells, providing a promising new therapeutic strategy for lung cancer treatment.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • GLI1 (GLI Family Zinc Finger 1) • HMGA2 (High mobility group AT-hook 2) • MMP9 (Matrix metallopeptidase 9)
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arsenic trioxide • Noxafil (posaconazole)
24d
Posaconazole for Pulmonary Fungal Infection Prophylaxis in Hematopoietic Stem Cell Transplantation Patients (clinicaltrials.gov)
P=N/A, N=360, Completed, Institute of Hematology & Blood Diseases Hospital, China | Not yet recruiting --> Completed
Trial completion
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Noxafil (posaconazole)
1m
New trial
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Noxafil (posaconazole)
1m
A multicenter, randomized controlled phase II clinical study of oral posaconazole combined with chemotherapy and PD-1 inhibitors as neoadjuvant treatment for early or locally advanced triple-negative breast cancer (ChiCTR2500098742)
P=N/A, N=40, Recruiting, Cancer Hospital of Shandong First Medical University (Shandong Cancer institute, Shandong Cancer Hospital); Cancer Hospital of Shandong First Medical | Not yet recruiting --> Recruiting
Enrollment open
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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HER-2 negative
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Noxafil (posaconazole)
2ms
A Phase 1 Dose-Escalation, Food Effect, and Drug-Drug Interaction Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the MALT1 Inhibitor, SGR-1505, in Healthy Volunteers. (PubMed, Clin Pharmacol Drug Dev)
Co-administration with posaconazole increased SGR-1505 exposure 3-fold...Asymptomatic, reversible indirect hyperbilirubinemia occurred, consistent with inhibition of UGT1A1. SGR-1505 was well-tolerated and exhibited favorable pharmacokinetic and pharmacodynamic properties, supporting further clinical development.
P1 data • PK/PD data • Journal
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IL2 (Interleukin 2) • MALT1 (MALT1 Paracaspase)
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Noxafil (posaconazole) • SGR-1505
3ms
Aminated Quinolinequinones With EDG(s) as a Prostate Cancer Inhibitor: Mechanistic Insights and Pharmacokinetic Limitations. (PubMed, Chem Biodivers)
In metabolic stability assays using human liver microsomes, AQQ6 exhibited relatively low intrinsic clearance (Clint) and an improved half-life (T1/2) compared to verapamil. However, pharmacokinetic studies in rats indicated poor oral bioavailability (%F = 4.2), likely due to extensive hepatic metabolism in rat liver microsomes. Molecular dynamics simulations targeting MAPK8, the protein likely involved in AQQ6 activity, were conducted to elucidate molecular-level binding interactions.
PK/PD data • Journal
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MAPK8 (Mitogen-activated protein kinase 8)
3ms
New P3 trial
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itraconazole • Noxafil (posaconazole)
3ms
Atrioventricular Block and Cluster Headache (SEVA) (clinicaltrials.gov)
P4, N=60, Active, not recruiting, Centre Hospitalier Universitaire de Nice | Recruiting --> Active, not recruiting | Trial completion date: Mar 2025 --> Sep 2027 | Trial primary completion date: Mar 2025 --> Sep 2025
Enrollment closed • Trial completion date • Trial primary completion date