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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
It is noteworthy that another family of SERMs typified by lasofoxifene and ormeloxifene (Figure 8.8) has been developed for estrogen-related therapeutic purposes. From a Structure-Activity Relationship (SAR) standpoint these agents are interesting as they contain three aromatic rings held in a similar rigid three-dimensional to those in the triphenylethylene analogues tamoxifen and toremifene. However, this is achieved through a central 1,2,3,4-tetrahydronaphthalene and chroman rings, respectively, rather than a double bond. Structures of the triphenylethylene-related SERMS lasofoxifene and ormeloxifene.
Abnormal uterine bleeding (the old dysfunctional uterine bleeding): How to manage?
Published in Carlos Simón, Linda C. Giudice, The Endometrial Factor, 2017
Hilary O. D. Critchley, Lucy Whitaker
Selective estrogen receptor modulators (SERMs) (for example, the SERM ormeloxifene) have been reported in early trials to show high efficacy in reducing HMB with a 97.7% reduction in PBAC at 4 months (105), but larger trials for this indication have not progressed.
PHBV/PLGA nanoparticles for enhanced delivery of 5-fluorouracil as promising treatment of colon cancer
Published in Pharmaceutical Development and Technology, 2020
Somayeh Handali, Eskandar Moghimipour, Mohsen Rezaei, Zahra Ramezani, Farid Abedin Dorkoosh
The presence of 5-FU in NPs was further confirmed by TGA analysis. As shown in Figure 4, three significant events of weight loss were occurred with increasing temperature. While in the 5-FU loaded NPs, the thermogram pattern was not changed significantly but a shift in the temperature (283, 364.4, and 487 °C to 294, 358, and 413 °C, respectively) was observed. Weight loss is also changed from 37.9, 68.2, and 93.1% to 59.3, 79.1, and 83.8%, respectively. This temperature shift may be due to the interaction between drug and polymeric NPs. The increase in weight loss of drug contaning NPs is attributed to the presence of 5-FU in the NPs. The rate of NPs degradation in the temperature range of 230 °C to 490 °C was slower than drug containing NPs. In other words, the loaded drug in the NPs led to decrease the stability of NPs, which may be due to interaction of drug with NPs. Difference in weight loss at temperatures about 480 to 600 °C (about 1% for NPs and 7% for 5-FU loaded NPs) are another indicators of 5-FU loading. Our findings are in agreement with Khan et al. (2015) results. They observed that weight loss of 55% and 80% for PLGA NPs and 74% and 95% for ormeloxifene loaded PLGP NPs. They indicated that greater weight loss was related to the presence of ormeloxifene in the NPs, which confirm the loading of the drug in NPs (Khan et al. 2015). Dubey et al. (2016) also reported that increase in weight loss of PLGA NPs was attributed to the presence of pentacyclic triterpenediol in the NPs, confirming the entrapment of the drug in the NPs (Dubey et al. 2016).