Acta Scientific Pharmaceutical Sciences

Mini Review Volume 8 Issue 11

Analytical Methods for the Estimation of Relugolix – A Review

Mukthinuthalapati Mathrusri Annapurna* and Pinninti Pradeep

Department of Pharmaceutical Analysis, GITAM School of Pharmacy, GITAM (Deemed to be University), Visakhapatnam, India

*Corresponding Author: Mukthinuthalapati Mathrusri Annapurna, Department of Pharmaceutical Analysis, GITAM School of Pharmacy, GITAM (Deemed to be University), Visakhapatnam, India.

Received: October 18, 2024; Published: October 28, 2024

Citation: Mukthinuthalapati Mathrusri Annapurna and Pinninti Pradeep. “Analytical Methods for the Estimation of Relugolix – A Review". Acta Scientific Pharmaceutical Sciences 8.11 (2024):39-40.

Abstract

Relugolix is used to treat advanced prostate cancer in men. Relugolix is used in the treatment of advanced hormone sensitive prostate cancer and also to manage heavy menstrual bleeding and severe pain. In the present study the authors have reviewed and summarised the analytical methods so far developed for the estimation of Relugolix in pharmaceutical formulations as well as biological fluids.

Keywords: Relugolix; Pain

Introduction

Relugolix (CAS: 737789-87-6) is chemically 1- [4- [1-[(2,6-difluoro phenyl) methyl]-5-[(dimethyl amino) methyl]-3-(6-methoxy pyridazin-3-yl)-2,4-dioxothieno[2,3-d] pyrimidin-6-yl] phenyl]-3-methoxy urea with molecular weight 623.6 g/mol. Relugolix is used in the treatment of advanced hormone sensitive prostate cancer [1] and also to manage heavy menstrual bleeding and severe pain [2-4]. Relugolix is soluble in organic solvents such as Ethanol, DMSO and dimethyl formamide and the solubility in these solvents is approximately 1, 20 and 25 mg/ml respectively and the pKa value is 8.63. Relugolix is a competitive antagonist of Gonadotropin-releasing hormone receptors, thereby decreasing the release of Luteinizing hormone and ultimately Testosterone. Relugolix is available as tablets with label claim 120 mg with brand names Rexigo (Zydus Cadila), R-Golix (Ipca Laboratories Ltd), OrgOnist (Sun Pharmaceuticals), Xelucip (Cipla Ltd) in India. The analytical methods such as UPLC-MS/MS [5], UPLC-MS [6], LC-MS/MS [7] RP-UPLC [8] RP-HPLC [9,10] were developed for the estimation of Relugolix and its impurities were studied by different authors in pharmaceutical dosage forms as well as biological fluids and some of the parameters were discussed in detail in Table 1.

Figure 1: Chemical structure of Relugolix (C29H27F2N7O5S).

Figure 1: Chemical structure of Relugolix (C29H27F2N7O5S).

Tucatinib is available as tablets with brand names Tucaxen 150 (Everest) Tukysa (Seetle Genetics), TukadxTM (Bigbear Pharmaceutical Laos) etc and label claim 150 mg. The analytical methods such as LC-MS/MS [4], UPLC-MS/MS [5], RP-HPLC [6,7] methods so far developed for the estimation of Tucatinib were given in Table 1.

Table 1: Review of analytical methods.

Table 1: Review of analytical methods.

Conclusion

The authors have briefly reviewed the analytical methods for the estimation of Relugolix in pharmaceutical dosage forms as well as biological fluids.

Bibliography

  1. Shore ND., et al. “Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer”. The New England Journal of Medicine 23 (2020): 2187-2196.
  2. Barra F., et al. “Relugolix for the treatment of uterine fibroids". Drugs of Today8 (2019): 503-512.
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  5. Liying Xing., et al. “An efficient UPLC-MS/MS Method established to detect Relugolix concentration in rat plasma”. Frontiers in Pharmacology 13 (2022): 874973.
  6. Thrinath SR., et al. “Development and validation of a method for studying Relugolix and its impurities by UPLC-MS”. Acta Chromatographica (2024).
  7. Siddhartha Lolla and Kumar Shiva Gubbiyapp. “Bio-analytical method development and validation for the quantitation of Relugolix in plasma samples by LC-MS/MS: application to bioavailability study in rabbits”. Rasayan Journal of Chemistry1 (2023): 494-501.
  8. Narayanareddy P and Ramakrishna Reddy K. “A novel validated stability indicative UPLC method for Relugolix for the determination of process-related and degradation impurities”. Rasayan Journal of Chemistry2 (2024): 325-336.
  9. Meruva Sathish Kumar., et al. “RP-HPLC method development and validation of Relugolix”. International Journal of Chemical and Biochemical Sciences6 (2023): 850-855.
  10. Mohan Pulletikurthi KVK., et al. “Force degradation studies of Relugolix: identification, isolation and structure characterization of stress degradation products by using liquid chromatography-mass spectrometry, auto purification mass mediated preparative-high performance liquid chromatography, high resolution mass spectrometry, nuclear magnetic resonance spectroscopy”. Spectroscopy Letters2 (2022): 128-137.

Copyright: © 2024 Mukthinuthalapati Mathrusri Annapurna and Pinninti Pradeep. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.