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DRUG CLASS:

Cytochrome P450 inhibitor

1d
New P3 trial
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itraconazole • Noxafil (posaconazole)
3d
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
7d
New trial
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Venclexta (venetoclax) • Noxafil (posaconazole)
1m
LSR overexpression induces chemoresistance in triple negative breast cancer cells through MDR1 upregulation and apoptosis attenuation. (PubMed, PLoS One)
MDR1 inhibitor verapamil and MDR1-targeted siRNA were used to evaluate the functional impact of LSR-induced MDR1. In contrast, knockout of LSR expression in MDA-MB-468 cells, which express higher levels of LSR, significantly sensitized the cells to doxorubicin-induced growth inhibition and apoptosis. Our data demonstrated that LSR overexpression promotes TNBC cell proliferation and invasion, and upregulation of MDR1 in these cells renders them resistant to doxorubicin, suggesting that targeting LSR could be a useful strategy to overcome chemoresistance in TNBC.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • LSR (Lipolysis Stimulated Lipoprotein Receptor)
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doxorubicin hydrochloride
1m
Characterizing CYP3A4-mediated drug interactions: a fixed-sequence pharmacokinetic Chinese study of posaconazole and ruxolitinib in haematological malignancies. (PubMed, J Antimicrob Chemother)
Although co-administration of posaconazole with ruxolitinib resulted in a statistically significant increase in ruxolitinib systemic exposure, the magnitude of this interaction was clinically moderate. Although ruxolitinib dose adjustment may not be routinely required when used concomitantly with posaconazole, close monitoring for ruxolitinib-related adverse effects is recommended under this combination therapy setting.
PK/PD data • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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Jakafi (ruxolitinib) • Noxafil (posaconazole)
1m
Design, Synthesis, and Biological Evaluation of Efflux-Resistant Imatinib Derivatives. (PubMed, J Med Chem)
Verapamil assays confirmed reduced efflux liability for compounds 8 and 13. Compound 8 also showed a positive therapeutic index. These findings support rational design to mitigate efflux-mediated resistance.
Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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imatinib
2ms
Cadmium Uptake into Rat Osteoblast UMR-106 Cells is Mediated via Multiple Pathways. (PubMed, Biol Trace Elem Res)
Treatment with verapamil, an L-type Ca2+ channel inhibitor, significantly reduced Cd uptake in UMR-106 cells...However, the degree of reduction ranged from 15 to 35%, indicating that no single pathway makes a predominant contribution. These findings suggest that diverse pathways, encompassing metal transporters and Ca2+ channels, contribute to Cd uptake in UMR-106 cells, although no single pathway predominates.
Preclinical • Journal
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CAV1 (Caveolin 1) • TRPV6 (Transient Receptor Potential Cation Channel Subfamily V Member 6) • CD2 (CD2 Molecule) • DMRT1 (Doublesex And Mab-3 Related Transcription Factor 1)
2ms
New trial
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Noxafil (posaconazole)
3ms
Posaconazole (MK-5592) Intravenous and Oral in Children (<2 Years) With Invasive Fungal Infection (MK-5592-127) (clinicaltrials.gov)
P2, N=40, Recruiting, Merck Sharp & Dohme LLC | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Dec 2026
Trial completion date • Trial primary completion date
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Noxafil (posaconazole)
3ms
New trial
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Noxafil (posaconazole)
4ms
New trial
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Noxafil (posaconazole)
4ms
Use of Adenosine to Determine the Electrophysiological Mechanism of Premature Ventricular Contractions (clinicaltrials.gov)
P4, N=100, Recruiting, Weill Medical College of Cornell University | Trial primary completion date: Jun 2025 --> Dec 2025
Trial primary completion date