Orgovyx (relugolix) / Intas, Gedeon Richter, Takeda, ASKA Pharma, Sumitomo Pharma, Pfizer, Knight Therap - LARVOL DELTA

Relugolix vs. Leuprolide in Combination with Radiotherapy for Localized Prostate Cancer: Analysis of Patient-Reported Quality of Life in a Randomized Trial (ASTRO 2026) - P2 | "In men receiving definitive RT plus ADT for localized prostate cancer, relugolix results in comparable short-term testosterone suppression with faster recovery and improved obstructive urinary, bowel, and vitality quality-of-life measures at 12 months versus leuprolide. These findings are exploratory and support prospective validation."

Clinical • Combination therapy • HEOR • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Baseline characteristics of patients (pts) enrolled in RENAISSANCE – A multicentre, non-interventional study of relugolix as androgen-deprivation therapy (ADT) in pts with hormone-sensitive prostate cancer (HSPC) (ESMO 2026) - No abstract available

Clinical • Observational data • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Oncology • Prostate Cancer • Solid Tumor

Effectiveness and Safety of Relugolix in Patients With Advanced Prostate Cancer Receiving Radiation Therapy: 6-Month Subgroup Analysis of the OPTYX Study (ASTRO 2026) - P | "In this 6-month subgroup analysis of the real-world OPTYX study, concurrent treatment with RT and relugolix was associated with testosterone suppression to castrate levels, low rates of SAEs, and high adherence at 6 months in patients with PC. This study is ongoing, and additional analyses are planned."

Clinical • Metastases • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Comparison of Patient-Reported Side Effects Between Leuprolide and Relugolix in Prostate Cancer Patients Receiving Radiation Therapy (ASTRO 2026) - "Overall post-ADT symptom burden was comparable between agents; however, differences in mood were observed beyond 6 months following treatment completion. Although relugolix and leuprolide have different mechanisms of action, whether there is a difference in quality-of-life impact post ADT cessation remains unclear."

Adverse events • Clinical • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Comparative Pharmacovigilance Analysis of Safety Signals Among Advanced Prostate Cancer Therapies Using FAERS (FDA Adverse Event Reporting System). (PubMed, Curr Oncol) - "A retrospective pharmacovigilance study of FAERS reports evaluated enzalutamide, darolutamide, apalutamide, abiraterone acetate, relugolix, niraparib/abiraterone, talazoparib, rucaparib, cabazitaxel, sipuleucel-T, and lutetium-177 vipivotide. The absence of a detected signal should not be interpreted as evidence of safety or equivalence, as reporting volume, detection bias, and statistical power varied across therapies. Overall, the therapies demonstrated distinct toxicity profiles, which may inform treatment selection, toxicity monitoring, and patient counseling."

Adverse events • Clinical • Journal • Retrospective data • Gastroenterology • Gastrointestinal Disorder • Genito-urinary Cancer • Hematological Disorders • Oncology • Prostate Cancer • Solid Tumor

Post-marketing safety profile of Myfembree in approved gynecologic indications: a disproportionality analysis based on the FAERS database. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Myfembree, a fixed-dose combination of relugolix, estradiol, and norethindrone acetate, is approved for premenopausal women with heavy menstrual bleeding associated with uterine fibroids and moderate to severe pain associated with endometriosis. These findings were generally consistent with the known safety profile of the drug and provide additional evidence on adverse event patterns and onset timing in routine gynecologic practice. Continued pharmacovigilance is warranted, particularly for thromboembolic events, blood pressure-related events, mood-related symptoms, and treatment-associated bleeding abnormalities."

Journal • P4 data • Alopecia • Cardiovascular • CNS Disorders • Depression • Endometriosis • Gynecology • Hematological Disorders • Immunology • Pain • Psychiatry • Pulmonary Embolism • Respiratory Diseases • Solid Tumor • Suicidal Ideation • Uterine Leiomyoma • Women's Health

Androgen Deprivation Therapy (Relugolix) for the Improvement of Diagnostic Imaging (PSMA PET/CT Scan) in Patients With High Risk or Very High Risk Prostate Cancer, The EnrichPSMA Trial (clinicaltrials.gov) - P2 | N=30 | Recruiting | Sponsor: Mayo Clinic | Trial completion date: Dec 2026 ➔ Mar 2029 | Trial primary completion date: Dec 2026 ➔ Jan 2029

Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Coronary Artery Plaque Progression After Androgen Deprivation Therapy in Men with Prostate Cancer: A Randomized Controlled Trial Comparing Relugolix Versus Leuprolide (SUO 2025) - P2 | "ADT for prostate cancer is associated with accelerated coronary atherosclerosis within 12 months and is higher with GnRH-agonist leuprolide compared with GnRH-antagonist relugolix."

Clinical • Acute Coronary Syndrome • Atherosclerosis • Coronary Artery Disease • Genito-urinary Cancer • Myocardial Infarction • Oncology • Prostate Cancer • Solid Tumor

Impact of Relugolix Versus Leuprolide on the Quality of Life of Men with Advanced Prostate Cancer: Results from the Phase 3 HERO Study. (PubMed, Eur Urol) - "Oral relugolix is a therapeutic option with similar patient-reported HRQOL to leuprolide, providing an oral option for androgen deprivation therapy associated with a more rapid testosterone reduction."

HEOR • Journal • Metastases • P3 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A multi-center, prospective, observational study of patients with prostate cancer being treated with relugolix: OPTYX. (ASCO-GU 2023) - P=N/A | "In the phase 3 HERO trial, relugolix maintained suppression of testosterone to castration levels in 96.7% of men from Day 29 to 48 weeks, with superiority to leuprolide acetate. In addition to assessing routine clinical care and disease progression, patient reported outcomes will be assessed with the Functional Assessment of Cancer Therapy-Prostate (FACT-P) for HRQoL and Simplified Medication Adherence Questionnaire (SMAQ) for adherence at 3 and 6 months then every 6 months. Clinical trial information: NCT05467176."

Clinical • Observational data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Safety and tolerability of relugolix in combination with abiraterone or apalutamide for treatment of advanced prostate cancer: Data from a 52-week clinical trial. (ASCO-GU 2025) - P1 | "REL used in combination with ABI or APA showed safety profiles consistent with individual drugs over 52 wks. REL levels were stable, and testosterone was sustained below castration level. These findings support the safety and tolerability of REL combination therapy with ABI or APA for aPC."

Clinical • Combination therapy • Metastases • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer. (PubMed, N Engl J Med) - P3 | "In this trial involving men with advanced prostate cancer, relugolix achieved rapid, sustained suppression of testosterone levels that was superior to that with leuprolide, with a 54% lower risk of major adverse cardiovascular events. (Funded by Myovant Sciences; HERO ClinicalTrials.gov number, NCT03085095.)."

Journal • P3 data • Cardiovascular • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Neoadjuvant darolutamide and relugolix combination preceding radical prostatectomy for high risk localized and locally advanced prostate cancer: A phase I/Ib trial. (ASCO-GU 2025) - P1 | "Blood, tumor and urine are stored for future correlative studies. The trial was activated in October 2024."

Clinical • Metastases • P1 data • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Quality of life, adherence, and adverse events among patients with advanced prostate cancer treated with relugolix: 6-month results of the OPTYX multicenter registry. (ASCO-GU 2026) - P | "Real-world utilization of relugolix was associated with stable QoL, high treatment adherence, and a low rate of serious AEs over the first 6 months. Patients will continue to be followed for a longer-term analysis in this ongoing study."

Adherence • Adverse events • Clinical • HEOR • Metastases • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Optyx study: Clinical characteristics and preferences for initiating relugolix in a cohort of US patients in real-world care settings. (ASCO-GU 2025) - P | "The OPTYX study enrolled 999 patients to assess real-world experience with relugolix. Nearly half started relugolix with other therapies. Many patients and physicians preferred the oral formulation, and other top reasons for initiation included safety and rapid testosterone suppression and recovery."

Clinical • Real-world • Real-world evidence • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Ultra-hypofractionated radiotherapy and concomitant oral relugolix for treatment of intermediate risk prostate cancer (ULTRA-HERO). (ASCO-GU 2026) - "Relugolix is an oral, highly selective, GnRH antagonist recently tested in a randomized phase III trial showing reduced risk in terms of cardiovascular events and rapid testosterone recovery if compared to Leuprolide. Enrollment started in May 2025 and 20 patients have been enrolled up to date. A final sample size of sample size of 73 patients will be needed to estimate the expected proportion of patients with complete biochemical response with a 5% precision margin and a 95% confidence interval."

Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Achieving Minimal-to-No Pain in Women with Endometriosis Treated with Relugolix Combination Therapy: SPIRIT Extension Trial. (PubMed, Int J Womens Health) - "Relugolix is an oral, non-peptide gonadotropin-releasing hormone receptor antagonist administered as once-daily combination therapy (relugolix-CT; 40 mg relugolix, 1 mg estradiol, 0.5 mg norethindrone acetate) to reduce endometriosis symptoms while potentially minimizing hypoestrogenic effects. Analgesic-free status improved in the placebo group after relugolix-CT initiation. In this post hoc analysis, women receiving relugolix-CT for up to 104 weeks had rapid dysmenorrhea improvement with amenorrhea and reduced analgesic use, with longer treatment associated with further NMPP reduction."

Journal • Endometriosis • Gynecology • Musculoskeletal Pain • Pain • Women's Health

Efficacy and Safety of Radiotherapy Plus Relugolix in Men With Localized or Advanced Prostate Cancer. (PubMed, JAMA Oncol) - "This multicenter post hoc analysis of patients with localized and advanced prostate cancer receiving radiotherapy in 2 randomized clinical trials (a phase 2 trial of relugolix vs degarelix, and a subset of the phase 3 HERO trial of relugolix vs leuprolide acetate) included men who were receiving radiotherapy and short-term (24 weeks) ADT (n = 103) from 2014 to 2015 and men receiving radiotherapy and longer-term (48 weeks) ADT (n = 157) from 2017 to 2019...Patients receiving longer-term ADT received relugolix, 120 mg, orally once daily (360-mg loading dose) or leuprolide acetate injections every 12 weeks for 48 weeks, with up to 90 days of follow-up...The results of these 2 randomized clinical trials suggest that relugolix rapidly achieves sustained castration in patients with localized and advanced prostate cancer receiving radiotherapy. No new safety concerns were identified when relugolix was used with radiotherapy."

Clinical • Journal • Metastases • Atrial Fibrillation • Cardiovascular • Genito-urinary Cancer • Hypertension • Oncology • Pain • Prostate Cancer • Solid Tumor

ENHANCE: Evaluating Hormone Therapy to Achieve Optimal Doses in Metastatic Prostate Cancer (clinicaltrials.gov) - P3 | N=1500 | Recruiting | Sponsor: University College, London | Not yet recruiting ➔ Recruiting

Enrollment open • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Short Course ADT for High Risk Low/Intermediate Risk ARTERA Prostate Cancer (clinicaltrials.gov) - P2 | N=90 | Recruiting | Sponsor: NYU Langone Health

New P2 trial • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A Phase I Clinical Trial Evaluating the Safety and Dosing of Relugolix with Novel Hormonal Therapy for the Treatment of Advanced Prostate Cancer. (PubMed, Target Oncol) - P1 | "Combination therapy of relugolix and abiraterone or apalutamide was associated with a favorable safety and tolerability profile consistent with the known profiles of the individual medications. Castration levels of testosterone were maintained after transitioning to relugolix from other ADTs."

Journal • Metastases • P1 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Safety and Tolerability of Relugolix in Combination with Abiraterone or Apalutamide for Treatment of Patients with Advanced Prostate Cancer: Data from a 52-Week Clinical Trial. (PubMed, Target Oncol) - P1 | "The safety/tolerability profile of both combination therapies was consistent with those of the individual drugs. These findings support using relugolix in combination with abiraterone or apalutamide as treatment of aPC."

Journal • Cardiovascular • Genito-urinary Cancer • Hypertension • Oncology • Prostate Cancer • Solid Tumor

Initial Results of a Phase 2 Trial of Stereotactic Body Radiation Therapy, Hormone/Androgen Deprivation Therapy and Radium 223 Dichloride for Oligometastatic Castrate Sensitive Prostate Cancer (SHARP) (ASTRO 2024) - P2 | "Materials/ ADT (degarelix [n=4], relugolix [n=2], or leuprolide [n=19]) was administered starting at least 4 weeks prior to SBRT and continued for 36 weeks. Ra-223 combined with SBRT to oligometastases and 36 weeks ADT in mCSPC is well-tolerated and results in favorable OS and PFS compared to historical controls. Longer follow-up is necessary to assess if the early use of Ra-223 delays development of new bone metastases."

Metastases • P2 data • Anemia • Cardiovascular • Gastroenterology • Genito-urinary Cancer • Hematological Disorders • Hepatology • Hypertension • Leukopenia • Metastatic Castration-Resistant Prostate Cancer • Musculoskeletal Diseases • Neutropenia • Oncology • Prostate Cancer • Solid Tumor • CXCL8 • TNFA

Targeting BCL-2 through Deep Learning-Based Drug Repurposing: A Multimodal Approach Combining Diffusion-Based Generative Modeling, Neural Relational Inference, and In Vitro Validation. (PubMed, J Chem Inf Model) - "We then extended NRI to protein-ligand trajectories to quantify residue-ligand and residue-residue dynamic couplings, enabling comparison of candidate-specific interaction signatures against the reference BCL-2 inhibitor Venetoclax. In vitro experiments supported BCL-2 inhibition by Relugolix in a TR-FRET assay and reduced viability of LN-18 glioma cells (IC50 = 23.55 μM). Together, these results establish a strategy that couples generative complex prediction with graph-based dynamic inference for structure-guided drug repurposing and identify Relugolix as a tractable scaffold for future BCL-2 inhibitor design."

Journal • Preclinical • Brain Cancer • Glioma • Oncology • Solid Tumor • BCL2

Testosterone suppression and recovery in patients with advanced prostate cancer treated with relugolix: an interim analysis of the OPTYX study (AUA 2026) - P | "Testosterone suppression in men treated with relugolix (monotherapy/combination) was sustained during treatment and recovered to baseline levels by 6 months after discontinuing treatment, while PSA remained stable. These findings support the testosterone suppression and recovery observed in the phase 3 HERO trial, supporting relugolix use in clinical practice."

Clinical • Metastases • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor