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DRUG CLASS:

Cytochrome P450 inhibitor

18d
Chemical components from Uncaria gambir (W.Hunter) Roxb. and their preliminary bioactivities in CDC25B phosphatase inhibition and vasodilatory activity. (PubMed, Nat Prod Res)
Compound 3 (3α-dihydrocadambine) effectively revealed strong vasodilatory activity with EC50 values of 2.4 μM and 2.1 μM, respectively, similar levels comparable to the positive control (verapamil)...Moreover, network pharmacology and molecular docking predicted compound 1 to correlate with the p53-Hippo-TGF-β antitumor signalling pathway and compound 3 with the cAMP/cGMP-PKG cardiovascular signalling pathway. This work provides preliminary experimental data for the development of potential lead compounds from U. gambir.
Journal
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TGFB1 (Transforming Growth Factor Beta 1) • CDC25B (Cell Division Cycle 25B) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)
19d
Amphotericin Versus Posaconazole for Pulmonary Mucormycosis (clinicaltrials.gov)
P2, N=82, Completed, Post Graduate Institute of Medical Education and Research, Chandigarh | Recruiting --> Completed | N=50 --> 82 | Trial completion date: Jul 2025 --> Feb 2026 | Trial primary completion date: Dec 2024 --> Feb 2026
Trial completion • Enrollment change • Trial completion date • Trial primary completion date
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Noxafil (posaconazole)
1m
Clinical impact of potential drug-drug interactions between midostaurin and posaconazole in FLT3-mutated AML. (PubMed, Antimicrob Agents Chemother)
Midostaurin clearance was delayed during co-administration. Midostaurin therapeutic drug monitoring may serve for decision-making when DDI with CYP3A4 inhibitors is suspected.
Journal
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FLT3 (Fms-related tyrosine kinase 3)
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FLT3 mutation
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midostaurin • Noxafil (posaconazole)
1m
Histoplasmosis Induction and Consolidation Therapy Factorial Randomized Clinical Trial (Histo-FACT) (clinicaltrials.gov)
P3, N=664, Not yet recruiting, University of Minnesota | Initiation date: May 2026 --> Sep 2026
Trial initiation date
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itraconazole • Noxafil (posaconazole)
2ms
Pharmacological boosting of azacitidine/venetoclax in acute myeloid leukemia. (PubMed, Blood Neoplasia)
Azacitidine/venetoclax is the standard treatment for patients with acute myeloid leukemia (AML) unfit for intensive chemotherapy. The potentiated antileukemic activity positions cobicistat as a promising complementary agent in AML therapy. This trial was registered at www.clinicaltrials.gov as NCT06014489.
Clinical • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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Venclexta (venetoclax) • azacitidine • Tybost (cobicistat)
2ms
Celastrol overcomes 5-fluorouracil resistance in osteosarcoma cells through p53-mediated apoptotic pathway modulation and P-glycoprotein inhibition: A comprehensive mechanistic study. (PubMed, Bioimpacts)
Celastrol reduced P-gp expression and increased intracellular drug accumulation, comparable to verapamil. Celastrol synergizes with 5-FU to overcome chemoresistance in osteosarcoma by enhancing p53-mediated and -independent apoptosis and inhibiting P-gp-mediated drug efflux. These findings suggest a promising low-toxicity therapeutic strategy, warranting further in vivo and clinical investigations.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP9 (Caspase 9)
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TP53 mutation
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5-fluorouracil
3ms
Co-encapsulated fluorescent magnetic nanoparticles for potential applications in breast cancer therapy: Exploratory in vitro and in vivo studies. (PubMed, Int J Pharm)
This study describes, for the first time in literature, a suitable approach to develop co-encapsulated magnetic nanoparticles based on fluorescent biotinylated N-palmitoyl chitosan, hydrophobic magnetite, Docetaxel and Verapamil. No significant toxicity was observed for magnetic nanoparticles in the rats. Overall, these findings suggest that the developed magnetic nanoplatforms represents a promising candidate for breast cancer applications and merits further in vivo investigation needed to elucidate the action mechanism of encapsulated therapeutics and their pharmacologic activity.
Preclinical • Journal
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CXCL8 (Chemokine (C-X-C motif) ligand 8)
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docetaxel
3ms
Simultaneous Determination of Venetoclax and Posaconazole in Human Plasma by UPLC-MS/MS: Application to Therapeutic Drug Monitoring in Acute Myeloid Leukemia Patients. (PubMed, Drug Des Devel Ther)
The trough concentrations of venetoclax were 9326.88 ± 12,169.05 ng/mL in patients treated with venetoclax alone, and 31,623.55 ± 28,453.67 ng/mL in patients treated with venetoclax in combination with posaconazole. A rapid and simple method was established and successfully applied to the simultaneous determination of the concentrations of venetoclax and posaconazole in AML patients, providing a basis for TDM and clinical pharmacokinetic analysis of these drugs in AML patients.
Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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Venclexta (venetoclax) • Noxafil (posaconazole)
3ms
KF2025#1 Trial: Ketamine, Cannabidiol and Cobicistat Interaction Study (clinicaltrials.gov)
P1, N=12, Not yet recruiting, Helsinki University Central Hospital
New P1 trial
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Tybost (cobicistat) • Epidiolex (cannabidiol)
3ms
New trial