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Conversion of Natural Products from Renewable Resources in Pharmaceuticals by Cytochromes P450
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Giovanna Di Nardo, Gianfranco Gilardi
Vitamin D2 (VD2) is physiologically produced from ergosterol in yeast or fungi, while VD3 is produced from 7-deoxycholesterol in mammals. The bioactive forms of vitamin D2 and D3, as well as their analogs, have been employed for the clinical treatment of different diseases including rickets, osteoporosis, hyperparathyroidism, and cancers. Paricalcitol (19-nor-1,25D2) and doxercalciferol (1α(OH)D2) that are vitamin D2 analogs, are currently used as drugs for the treatment of secondary hyperparathyroidism (Bover et al., 2014) and paricalcitol was shown to have anticancer activity (Alagbala et al., 2006; Chodyński et al., 2002).
Main Classes of Drugs
Published in Jerome Z. Litt, Neil H. Shear, Litt's Drug Eruption & Reaction Manual, 2017
Vitamin D receptor agonistDihydrotachysterolDoxercalciferolParicalcitol
Proteomics based drug repositioning applied to improve in vitro fertilization implantation: an artificial intelligence model
Published in Systems Biology in Reproductive Medicine, 2021
Roberto Matorras, Raquel Valls, Mikel Azkargorta, Jorge Burgos, Aintzane Rabanal, Felix Elortza, Jose Manuel Mas, Teresa Sardon
Among the drug candidates in Table 3, three vitamin D-related compounds, doxercalciferol, calcidiol, and dihydrotachysterol, were identified. The decidua produces calcitriol in response to IL-1B secreted by the blastocyst. It may help support implantation by attenuating decidual T-cell function (Barrera et al. 2015; Thangamani et al. 2015). Decidual NK cells treated with calcitriol show decreased cytokine synthesis, such as IL-6 and TNFα, which are linked to pregnancy failure (Tamblyn et al. 2015). Additionally, vitamin D may play an important autocrine role through its regulation of the transcription of genes such as HOXA10, critical for EI and placentation (Evans et al. 2004). Several studies have shown worse IVF outcomes in women with deficient vitamin D levels (Chu et al. 2018; Iliuta et al. 2020), and vitamin D supplementation is recommended in IVF deficient and insufficient women (Chu et al. 2018; Iliuta et al. 2020).
Inhibitory effect of sixteen pharmaceutical excipients on six major organic cation and anion uptake transporters
Published in Xenobiotica, 2021
Ruicong Ma, Gentao Li, Xue Wang, Yajuan Bi, Youcai Zhang
Tween 80 is used in injectable formulations of amiodarone, calcitriol, chlordiazepoxide, docetaxel (substrate of hOATP1B3), doxercalciferol and etoposide (substrate of hOATP1B3), as well as oral formulations of doxycycline, tramadol, and acetaminophen (inhibitor of hOAT1) (Apiwattanakul et al., 1999; Strickley, 2004). The current data suggest that Tween 80 is a strong inhibitor of hOAT3. Tween 80 was reported to inhibit the urinary excretion of methotrexate (Azmin et al., 1985). This might be due to the inhibitory effect of Tween 80 on hOAT3, which has been shown to transport methotrexate with a high affinity (Iwaki et al., 2017). Taxotere, an intravenous drug containing active substance docetaxel, contains 55 mg/kg Tween 80 per dose, leading to a plasma concentration of 550 μg/mL (50 kg adult; 5 liters effective circulating blood volume) (ten Tije et al., 2003). At this concentration, the [I]/IC50 values of Tween 80 for hOCT2, hOAT1, hOAT3, and hOATP1B3 are much higher than 0.1. Thus, the potential Tween 80–drug interactions should be further investigated.
Evaluating extended-release calcifediol as a treatment option for chronic kidney disease-mineral and bone disorder (CKD-MBD)
Published in Expert Opinion on Pharmacotherapy, 2019
Mario Cozzolino, Markus Ketteler
Calcitriol and other active (1α-hydroxylated) vitamin D analogues, such as paricalcitol, alfacalcidol, or doxercalciferol, are another treatment option for SHPT in ND-CKD patients. Although RCTs show active vitamin D and its analogues can effectively suppress PTH levels in ND-CKD, these agents are associated with an increased risk of hypercalcemia due to their effects on increasing intestinal calcium absorption [52–54]. As a consequence, the 2017 CKD-MBD KDIGO guideline recommends that these agents should not be routinely used in ND-CKD patients. Instead, their use should be restricted to patients with stage 4 and 5 CKD who have severe and progressive hyperparathyroidism [55]. Active vitamin D analogues have also been associated with increased intestinal absorption of phosphorus, which can potentially result in hyperphosphatemia. This potential combination of hyperphosphatemia and hypercalcemia with active vitamin D analogues increases the risk of vascular calcification [56].