Darolutamide
- Generic Name
- Darolutamide
- Brand Names
- Nubeqa
- Drug Type
- Small Molecule
- Chemical Formula
- C19H19ClN6O2
- CAS Number
- 1297538-32-9
- Unique Ingredient Identifier
- X05U0N2RCO
- Background
Darolutamide is a nonsteroidal androgen receptor antagonist for the treatment of castrate-resistant, non-metastatic prostate cancer (nmCRPC). This condition occurs in the majority of patients with advanced prostate cancer who have been treated with androgen receptor antagonists. Though prior treatment for prostate cancer has been successful for these patients, the cancer eventually progresses to become resistant to existing therapies. This warrants further treatment.
The goal of treatment with darolutamide is to delay the progression of prostate cancer to metastatic disease, increasing quality of life and life expectancy for those with advanced prostate cancer. Darolutamide was developed by Bayer HealthCare Pharmaceuticals Inc. and approved by the FDA on July 30th, 2019.
- Indication
Darolutamide is indicated for the treatment of adults with non-metastatic castration-resistant prostate cancer (nmCRPC) and metastatic hormone-sensitive prostate cancer (mHSPC) in combination with docetaxel.
- Associated Conditions
- Metastatic Hormone-Sensitive Prostate Cancer (mHSPC), Non-Metastatic Castration-Resistant Prostate Cancer
G8 Frailty Assessment Tool Predicts Docetaxel Tolerability in Metastatic Prostate Cancer
• A multicenter retrospective study reveals frailty assessments, particularly the G8 screening tool, can effectively identify metastatic prostate cancer patients at higher risk for severe adverse events from docetaxel treatment.
• Among 32 evaluated patients, 56% experienced severe adverse events, with significant correlations found between these events and lower G8 scores (P<.001), BMI (P=.011), and serum albumin levels (P=.046).
• Researchers developed a predictive nomogram showing patients with a G8 score of 12 had a 73% probability of experiencing severe docetaxel-related adverse events, suggesting potential need for treatment intensity modifications.
Pfizer to Showcase Breakthrough Cancer Therapies at ASCO 2025 with Over 60 Presentations
• Pfizer will present data from more than 60 abstracts at ASCO 2025, including 15 oral presentations highlighting advancements across breast, genitourinary, hematologic, thoracic, and colorectal cancers.
• Two late-breaking presentations will be featured in ASCO's press program, including pivotal survival data for BRAFTOVI in colorectal cancer and progression-free survival results for vepdegestrant in metastatic breast cancer.
• The company will showcase novel antibody-drug conjugate combinations with immunotherapy and present five-year survival data for XTANDI in prostate cancer, supporting Pfizer's goal of delivering eight breakthrough cancer medicines by 2030.
Vividion Therapeutics Initiates Phase I Trial of Novel RAS-PI3Kα Inhibitor for Advanced Solid Tumors
• Vividion Therapeutics has dosed the first patient in a Phase I trial of VVD-159642, an oral inhibitor targeting the RAS-PI3Kα pathway implicated in approximately 20% of all cancers.
• The study will evaluate VVD-159642 as both monotherapy and in combination with sotorasib or trametinib in patients with advanced solid tumors, potentially offering a new treatment approach for RAS-driven cancers.
• VVD-159642 represents Vividion's fourth clinical-stage program from its chemoproteomics platform, designed to selectively inhibit oncogenic signaling while avoiding toxicities that have limited previous attempts to target this pathway.
CD46-Targeting ADC FG-3246 Shows Promising Results in Advanced Prostate Cancer Trial
• FG-3246, a first-in-class antibody-drug conjugate targeting CD46, demonstrated an 80% disease control rate and 20% objective response rate in heavily pre-treated metastatic castration-resistant prostate cancer patients.
• The phase 1 trial established 2.7 mg/kg as the maximum tolerated dose, with manageable safety profile including neutropenia as the most common adverse event, while showing a median radiographic progression-free survival of 8.7 months.
• FibroGen plans to advance FG-3246 with a phase 2 monotherapy study by mid-2025 and will disclose results from a combination trial with enzalutamide in the second half of 2025.
Pathos AI Initiates Phase 1b/2a Trial of Pocenbrodib for Metastatic Castration-Resistant Prostate Cancer
• Pathos AI has dosed the first patient in a Phase 1b/2a trial evaluating pocenbrodib, a CBP/p300 inhibitor, alone and in combination with established therapies for metastatic castration-resistant prostate cancer.
• The multicenter trial will enroll approximately 203 patients who have progressed despite prior therapy, with primary objectives to assess safety, response rates, and determine recommended Phase 2 dosing.
• Pocenbrodib targets underlying resistance mechanisms to AR-targeted therapy through CBP/p300 inhibition, addressing a significant unmet need in advanced prostate cancer treatment.
Darolutamide Demonstrates Superior Benefits in Black and White Patients with Non-Metastatic Prostate Cancer
• Real-world evidence from the DEAR study reveals darolutamide offers longer treatment duration and delayed progression compared to enzalutamide and apalutamide in non-metastatic castration-resistant prostate cancer patients.
• Among 1,205 patients studied, darolutamide showed lower discontinuation rates (32.8% Black, 37.9% White) compared to enzalutamide (44.8% Black, 53.1% White) and apalutamide (48.8% Black, 50.4% White).
• Median metastasis-free survival was not reached in the darolutamide group for both racial cohorts, while enzalutamide and apalutamide groups showed shorter survival periods.
NUBEQA Shows Strong Efficacy in Metastatic Prostate Cancer Subgroups, New Trial Data Reveals
• New ARANOTE trial data demonstrates NUBEQA plus ADT reduced risk of disease progression by 70% in low-volume metastatic hormone-sensitive prostate cancer patients and 40% in high-volume disease patients.
• Subgroup analysis of ARASENS trial confirms NUBEQA's benefits across age groups, showing consistent survival improvements in both patients under and over 75 years old.
• Real-world analysis indicates NUBEQA combination therapy results in lower treatment discontinuation rates and better PSA responses compared to alternative treatments.
Pfizer to Present Landmark Survival Data for Cancer Therapies at ASCO GU 2025 Symposium
• Pfizer will showcase over 20 abstracts at ASCO GU 2025, including pivotal Phase 3 TALAPRO-2 trial results demonstrating significant overall survival benefits for TALZENNA-XTANDI combination in prostate cancer.
• Updated analysis from Phase 3 EV-302 trial confirms sustained survival advantage of PADCEV with pembrolizumab in advanced urothelial cancer, reinforcing its position as a first-line treatment standard.
• Novel investigational therapy mevrometostat shows promising progression-free survival data when combined with XTANDI in metastatic castration-resistant prostate cancer, advancing Pfizer's genitourinary cancer pipeline.
J&J Seeks FDA Approval for TAR-200 in BCG-Unresponsive Non-Muscle Invasive Bladder Cancer
• Johnson & Johnson has initiated a New Drug Application (NDA) submission to the FDA for TAR-200.
• TAR-200 is intended for patients with Bacillus Calmette-Guérin (BCG)-unresponsive high-risk non-muscle-invasive bladder cancer (HR-NMIBC).
• Phase 2b SunRISe-1 study data showed an 83.5% complete response rate with TAR-200 monotherapy.
• The FDA is reviewing the application under the Real-Time Oncology Review (RTOR) program to expedite potential approval.
Treatment Selection Criteria Evolves for Metastatic Hormone-Sensitive Prostate Cancer: Expert Insights
• High-volume metastatic prostate cancer is characterized by visceral metastases or multiple bone lesions, with patients typically surviving 3-4 years after initial diagnosis.
• Treatment decisions are increasingly personalized, with younger patients showing liver metastases being considered for triplet therapy based on the ARASENS trial findings.
• Most patients receive doublet therapy with ADT plus apalutamide or enzalutamide, while darolutamide emerges as an alternative for patients on blood thinners.
ORIC Pharmaceuticals Announces Promising Early Data for ORIC-944 and Collaboration for ORIC-114
• ORIC Pharmaceuticals reported encouraging early data from a Phase 1b trial of ORIC-944 combined with apalutamide in metastatic castration-resistant prostate cancer (mCRPC).
• The company entered a clinical trial collaboration with Johnson & Johnson to evaluate ORIC-114 with amivantamab for first-line treatment of NSCLC with EGFR exon 20 insertion mutations.
• ORIC anticipates seven data readouts across ORIC-114 and ORIC-944 programs in the next 18 months, potentially leading to registrational trials in 2025 and 2026.
Bayer Seeks Approval in China for Darolutamide to Treat Metastatic Hormone-Sensitive Prostate Cancer
• Bayer has submitted an application to China's NMPA for darolutamide, seeking its approval in combination with androgen deprivation therapy (ADT) for mHSPC.
• The application is based on the Phase III ARANOTE trial, which demonstrated a 46% reduction in the risk of radiological progression or death compared to placebo plus ADT.
• Darolutamide, marketed as Nubeqa®, is already approved in China for mHSPC with ADT and docetaxel, and for nmCRPC at high risk of metastatic disease.
• The ARANOTE trial's results showed a significant extension in radiological progression-free survival (rPFS) with darolutamide plus ADT, benefiting various patient subgroups.
Bayer's BAY 2927088 Advances to Phase 3 Trial for HER2-Mutated NSCLC
• Bayer has initiated a Phase 3 trial (SOHO-02) for BAY 2927088 as a first-line treatment for HER2-mutated non-small cell lung cancer (NSCLC).
• The trial will compare BAY 2927088 to pembrolizumab with chemotherapy, the current standard of care for this specific type of lung cancer.
• BAY 2927088, an oral drug inhibiting both HER2 and EGFR, has received breakthrough therapy designations in the US and China as a second-line treatment.
• Bayer is also due to present results from the phase 1/2 SOHO-01 study of BAY 2927088 as a second-line therapy for HER2-altered NSCLC at the World Conference on Lung Cancer (WCLC).
Pharma Stock Roundup: Novo Nordisk's Obesity Study Disappoints, Lilly's Zepbound Approved for Sleep Apnea
• Novo Nordisk's CagriSema obesity treatment showed a 22.7% weight loss in Phase III, falling short of the anticipated 25% reduction, impacting stock prices.
• Eli Lilly's Zepbound (tirzepatide) received FDA approval for moderate-to-severe obstructive sleep apnea (OSA), marking it as the first drug for obesity-related OSA.
• AstraZeneca and Daiichi Sankyo withdrew their EU application for Dato-DXd in non-small cell lung cancer (NSCLC) but pursue U.S. approval for EGFR-mutated NSCLC.
• Pfizer's Braftovi gained FDA approval in combination with Erbitux and mFOLFOX6 for first-line treatment of metastatic colorectal cancer with BRAF mutations.
Nuvation Bio's Taletrectinib Gains FDA Priority Review and Expanded Access Program for ROS1+ NSCLC
• The FDA granted priority review to Nuvation Bio's NDA for taletrectinib, a next-generation ROS1 inhibitor, for advanced ROS1+ non-small cell lung cancer, setting a PDUFA date of June 23, 2025.
• Taletrectinib demonstrated promising efficacy and tolerability in the TRUST-I and TRUST-II trials, showing durable responses and prolonged progression-free survival in ROS1+ NSCLC patients.
• Nuvation Bio has initiated an Expanded Access Program (EAP) in the U.S. for taletrectinib, offering access to eligible patients with advanced ROS1+ NSCLC outside of clinical trials.
• The NDA is based on pooled data from the TRUST-I and TRUST-II studies, which included over 300 patients, representing the largest ROS1-positive NSCLC dataset supporting an NDA.
Acoramidis Gains Global Momentum: FDA Approval, EU Recommendation, and Promising Clinical Data
• Acoramidis (Attruby), developed by Stanford Medicine and BridgeBio, receives FDA approval for transthyretin amyloid cardiomyopathy (ATTR-CM) treatment, marking a significant milestone.
• The European Medicines Agency's CHMP recommends acoramidis for EU marketing authorization based on positive Phase 3 ATTRibute-CM trial results.
• Clinical trials demonstrate acoramidis' efficacy in reducing cardiovascular-related hospitalizations and improving survival rates for ATTR-CM patients.
• Bayer and BridgeBio collaborate to commercialize acoramidis, with Bayer holding EU rights and plans for a launch in Europe in early 2025.
Advances in Metastatic Prostate Cancer: Novel Treatment Strategies Emerge
• The ARANOTE trial demonstrated that darolutamide plus ADT significantly improves radiographic progression-free survival in mHSPC patients.
• PEACE-3 trial results highlighted that combining radium-223 with enzalutamide significantly improved outcomes in mCRPC patients with bone metastases.
• SPLASH trial data suggests 177Lu-PNT2002 may offer a new radioligand therapy option for mCRPC patients who have progressed after an ARPI.
FDA Accepts Bayer's Nubeqa sNDA for Metastatic Hormone-Sensitive Prostate Cancer
• The FDA has accepted Bayer's sNDA for Nubeqa (darolutamide) in combination with androgen deprivation therapy (ADT) for mHSPC.
• The sNDA is based on positive Phase III ARANOTE trial results, demonstrating improved radiological progression-free survival (rPFS).
• If approved, Nubeqa would offer an additional treatment option for mHSPC patients, both with and without chemotherapy.
• GlobalData estimates Nubeqa sales could reach $3.6 billion by 2029, highlighting its potential impact on prostate cancer treatment.
Bayer Seeks EU Approval for Nubeqa in Metastatic Hormone-Sensitive Prostate Cancer
• Bayer has submitted an application to the European Union for approval of Nubeqa (darolutamide) for metastatic hormone-sensitive prostate cancer (mHSPC).
• The application is based on Phase III ARANOTE trial data, which demonstrated a significant extension in radiographic progression-free survival (rPFS) when Nubeqa was combined with hormone therapy.
• Nubeqa is already approved for mHSPC in combination with hormone therapy and chemotherapy, as well as for non-metastatic castration-resistant prostate cancer.
• Nubeqa's sales are projected to exceed one billion in 2024, reflecting its growing use in prostate cancer treatment.
Bayer Seeks FDA Approval to Expand Nubeqa's Indication for Metastatic Hormone-Sensitive Prostate Cancer
• Bayer has submitted a supplemental New Drug Application (sNDA) to the FDA for Nubeqa (darolutamide) in combination with androgen deprivation therapy (ADT).
• The sNDA is seeking approval for the treatment of patients with metastatic hormone-sensitive prostate cancer (mHSPC), expanding its current indications.
• The submission is based on positive results from the Phase III ARANOTE trial, which were presented at the 2024 ESMO Congress and published in The Journal of Clinical Oncology.
• Nubeqa, an oral androgen receptor inhibitor (ARi), is jointly developed by Bayer and Orion Corporation.
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