更新于：2024-12-21
Apalutamide
阿帕他胺
更新于：2024-12-21
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2018-02-14), |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、临床急需境外新药 (中国)、优先审评 (澳大利亚) |
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结构
分子式C21H15F4N5O2S |
InChIKeyHJBWBFZLDZWPHF-UHFFFAOYSA-N |
CAS号956104-40-8 |
关联
150
项与 阿帕他胺 相关的临床试验A Randomized Trial of Apalutamide in Non-Muscle Invasive Bladder Cancer
A Randomized Clinical Trial for the Addition of Docetaxel to Androgen Receptor Pathway Inhibitors in Patients With Metastatic Castration Sensitive Prostate Cancer Without Deep PSA Response
PROSTATE-IQ: Parallel RandOmized STudy of Personalized Apalutamide Treatment and Evaluation to Improve Quality of Life in Post-Operative Radiation With Androgen Axis Suppression. A Phase III Multi-center Study for Men With Detectable PSA After Prostatectomy for Prostate Cancer.
100 项与 阿帕他胺 相关的临床结果
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100 项与 阿帕他胺 相关的转化医学
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100 项与 阿帕他胺 相关的专利（医药）
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567
项与 阿帕他胺 相关的文献（医药）2025-02-01PROSTATE
Efficacy and Predictive Factors Analysis of Androgen Deprivation Plus Novel Hormone Therapy as Neoadjuvant Treatment for High‐Risk Prostate Cancer
Article
作者: Dong, Liang ; Tao, Hanyang ; Pan, Jiahua ; Du, Xinxing ; Li, Rui ; Wu, Fan ; Xue, Wei ; Dong, Baijun ; Zhu, Yinjie
ABSTRACT:
Background:
This investigation explored the clinical features, pathological outcomes, and biochemical recurrence (BCR) duration among high‐risk prostate cancer (HRPC) patients who have undergone neoadjuvant therapy (NAT) in combination with radical prostatectomy (RP) and pelvic lymph node dissection (PLND). Additionally, we identified prognostic indicators that discern pathological complete response (pCR) or minimal residual disease (MRD) and BCR.
Methods:
In total, we examined 76 HRPC patients, who received NAT with either androgen deprivation therapy (ADT) plus apalutamide or ADT plus abiraterone, with subsequent RP and PLND. We conducted a genetic evaluation of patients receiving neoadjuvant apalutamide. Additionally, patient pathological outcomes, circulating prostate‐specific antigen (PSA) response rates, and BCR duration were analyzed. Lastly, we employed uni‐ and multivariate analyses to screen for prognostic factors that govern pCR or MRD and BCR duration.
Results:
Patient median age and median PSA at presentation were 69 years (IQR: 66–73), and 47.6 ng/mL (IQR: 24.1–105.75), respectively. We observed marked changes in pCR or MRD rates between the two cohorts. In particular, the ADT plus apalutamide cohort (51.5%) exhibited enhanced rates relative to the ADT plus abiraterone cohort (25.6%) (p = 0.03). The median BCR duration was substantially prolonged among neoadjuvant apalutamide cohort relative to the neoadjuvant abiraterone cohort (261 days vs. 76 days, p = 0.04). Using multivariate analysis, we revealed that the postintervention pre‐RP PSA content (≤ 0.1 ng/mL vs. > 0.1 ng/mL) remained a substantial stand‐alone indicator of pCR or MRD (odds ratio: 10.712, 95% CI: 2.725–42.105, p < 0.001). Furthermore, supplemental analyses revealed that the ADT plus apalutamide cohort exhibited an augmented serum response rate, which, in turn, reduced the post‐intervention pre‐RP PSA content. Based on our genetic profiling of the neoadjuvant apalutamide cohort demonstrated high‐frequency deleterious changes in the AR axis (30.3%), followed by TP53 mutations (15.15%). Patients with defective AR axis experienced a remarkably shorter median BCR duration relative to patients with other or no genetic alterations (52.5 days vs. 286 and 336 days, respectively, p < 0.0001). Furthermore, using multivariate analysis, we demonstrated that achieving pCR or MRD (hazard ratio [HR]: 0.170, 95% CI: 0.061–0.477, p < 0.001) and presence of defective AR signaling (HR: 11.193, 95% CI: 3.499–35.806, p < 0.001) were strong stand‐alone indicators of BCR.
Conclusions:
Herein, we demonstrated the superior performance of ADT plus apalutamide in achieving pCR or MRD and in extending BCR duration among HRPC patients. Post‐intervention pre‐RP PSA content as well as genetic shifts, especially in the AR axis, are critical indicators of patient pathological and clinical outcomes. These findings highlight the significance of genetic testing and PSA content monitoring in treating HRPC patients.
2025-02-01PROSTATE
Comparison of abiraterone, enzalutamide, and apalutamide for metastatic hormone‐sensitive prostate cancer: A multicenter study
Article
作者: Kimura, Takahiro ; Yanagisawa, Takafumi ; Urabe, Fumihiko ; Katsumi, Kouta ; Iwatani, Kosuke ; Tashiro, Kojiro ; Habuchi, Tomonori ; Takahashi, Hidetsugu ; Mori, Keiichiro ; Shimomura, Tatsuya ; Narita, Shintaro ; Hatakeyama, Shingo ; Muramoto, Katsuki ; Fukuokaya, Wataru
Abstract:
Purpose:
We aimed to assess the differential efficacy and safety of androgen receptor pathway inhibitors (ARPI), such as abiraterone, enzalutamide, and apalutamide, in patients with metastatic hormone‐sensitive prostate cancer (mHSPC) in a real‐world practice setting.
Methods:
We retrospectively reviewed the records of consequent 668 patients with mHSPC treated with ARPI plus androgen deprivation therapy between September 2015 and December 2023. Based on the LATITUDE criteria, the comparison among abiraterone, enzalutamide, and apalutamide was exclusively conducted in high‐risk patients. Prostate‐specific antigen (PSA) responses such as the achievement of 95% and 99% PSA decline, overall survival (OS), cancer‐specific survival (CSS), time to castration‐resistant prostate cancer (CRPC), and the incidence of adverse events (AEs) were compared. All two‐group comparisons relied on propensity score matching (PSM) to minimize the effect on possible confounders.
Results:
In total, 297 patients with high‐risk mHSPC treated with abiraterone, 127 with enzalutamide, and 142 with apalutamide were compared. There were no differences in time to CRPC (p = 0.13), OS (p = 0.7), and CSS (p = 0.5) among the three ARPIs. No differences were observed in the achievement rates for 95% PSA decline at 3 months among the three ARPIs, while abiraterone was significantly better in 99% PSA decline achievement compared to apalutamide (72% vs. 57%, p = 0.003). The aforementioned oncologic outcomes were sustained even when performing PSM analyzes. Although skin rash for APA (34%) was the highest incidence of AEs, there were no differences in the rates of severe AEs across the three ARPIs. Enzalutamide resulted in the lowest treatment discontinuation rates (10%) other than disease progression compared to the other regimens.
Conclusions:
Abiraterone, enzalutamide, and apalutamide have comparable oncologic outcomes in terms of OS, CSS, and time to CRPC in patients with high‐risk mHSPC. Our data on differential treatment discontinuation rates, PSA response, and AE profiles can help guide clinical decision‐making.
2025-02-01Clinical Genitourinary Cancer
Dose Per Body Weight Predicts Incidence and Severity of Apalutamide-Related Skin Rash in Metastatic Castration-Sensitive Prostate Cancer
Article
作者: Nakano, Yuzo ; Teishima, Jun ; Miyake, Hideaki ; Shiraishi, Yusuke ; Chiba, Koji ; Terakawa, Tomoaki ; Okamura, Yasuyoshi ; Suzuki, Kotaro ; Hyodo, Yoji ; Okada, Keisuke ; Hara, Takuto ; Bando, Yukari
BACKGROUND:
A survival advantage with apalutamide (APA) combined with androgen deprivation therapy for metastatic castration-sensitive prostate cancer (mCSPC) has been demonstrated in the clinical trial, irrespective of race. However, the incidence of APA-induced skin rash in the Japanese subpopulation is higher than that in the global population. In the present study, we investigated the predictive value of APA dose per body weight for the incidence of skin rash.
METHODS:
A total of 128 patients with mCSPC treated with APA between January 2018 and December 2022 were retrospectively reviewed. A receiver operating characteristic analysis was performed to identify the optimal APA cutoff dose. In addition to comparing the status of APA-induced skin rash, the progression-free survival (PFS) was compared after propensity score matching.
RESULTS:
The optimal cutoff dose predicting the occurrence of skin rash was 3.33 mg/kg. Our cutoff value significantly stratified the 2 groups in time to occurrence of APA-induced skin rash and discontinuation of APA due to skin rash (P = .005 and P = .009, respectively). The incidence of a ≥G3 skin rash in patients receiving ≥3.33 mg/kg was significantly higher than in others (6.5% vs. 19.7%, P = .037). There was no significant difference in the PFS between patients administered <3.33 mg/kg and those administered ≥3.33 mg/kg.
CONCLUSIONS:
Our data suggest that the drug dosage per body weight may predict the incidence and severity of APA-induced skin rash. Further large-scale prospective studies are needed to validate the predictive value of drug dosage per body weight and identify the optimal cutoff value.
233
项与 阿帕他胺 相关的新闻（医药）2024-12-20
核酸药物申请上市
2024-12-20
临床研究免疫疗法临床申请
2024-12-18
加速审批临床结果
100 项与 阿帕他胺 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 转移性前列腺癌 | 日本 | 2020-05-29 | |
| 转移性去势抵抗性前列腺癌 | 美国 | 2019-09-17 | |
| 激素依赖性前列腺癌 | 欧盟 | 2019-01-14 | |
| 激素依赖性前列腺癌 | 冰岛 | 2019-01-14 | |
| 激素依赖性前列腺癌 | 列支敦士登 | 2019-01-14 | |
| 激素依赖性前列腺癌 | 挪威 | 2019-01-14 | |
| 前列腺癌 | 加拿大 | 2018-07-27 | |
| 去势敏感前列腺癌 | 澳大利亚 | 2018-07-05 | |
| 去势抵抗性前列腺癌 | 美国 | 2018-02-14 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 非转移性前列腺癌 | 临床3期 | 法国 | 2020-01-09 | |
| 晚期前列腺癌 | 临床3期 | 美国 | 2015-11-20 | |
| 晚期前列腺癌 | 临床3期 | 美国 | 2015-11-20 | |
| 晚期前列腺癌 | 临床3期 | 美国 | 2015-11-20 | |
| 晚期前列腺癌 | 临床3期 | 阿根廷 | 2015-11-20 | |
| 晚期前列腺癌 | 临床3期 | 阿根廷 | 2015-11-20 | |
| 晚期前列腺癌 | 临床3期 | 阿根廷 | 2015-11-20 | |
| 晚期前列腺癌 | 临床3期 | 比利时 | 2015-11-20 | |
| 晚期前列腺癌 | 临床3期 | 比利时 | 2015-11-20 | |
| 晚期前列腺癌 | 临床3期 | 比利时 | 2015-11-20 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | prostate-specific antigen | - | 製膚鑰網衊築膚獵積選(蓋繭衊遞觸網窪簾築鑰): HR = 0.24 (95% CI, 0.13 ~ 0.43), P-Value = <0.001 更多 | 积极 | 2024-12-01 | ||
Placebo | |||||||
临床2期 | 108 | (Apalutamide Plus ADT (Main Study) + Relugolix Followed by Apalutamide Plus Relugolix (Sub Study)) | 壓願夢糧廠觸淵壓範築(襯鹹衊襯鹹選衊壓夢鏇) = 膚淵壓積獵膚鏇夢積製 窪獵衊廠鏇觸選網鏇遞 (艱蓋艱衊構襯繭餘廠膚, 蓋膚網獵醖鬱顧憲襯膚 ~ 壓製積製鏇膚鹽顧鑰鬱) 更多 | - | 2024-11-19 | ||
(Sub Study: Relugolix Followed by Apalutamide Plus Relugolix) | 壓窪衊淵願壓蓋繭鹹觸(艱積鏇鑰夢醖鏇鹽襯齋) = 廠願範廠簾糧襯廠遞遞 鏇淵衊糧鹽鏇鬱壓鏇願 (積襯製餘襯鬱襯蓋糧衊, 簾鬱夢構觸製餘網遞鏇 ~ 簾襯餘夢膚餘淵鏇繭餘) 更多 | ||||||
临床3期 | 1,179 | 餘鹽膚壓壓憲憲鏇積網(製顧鑰築觸衊鬱窪餘願): HR = 0.22 (95% CI, 0.17 ~ 0.27) 更多 | 积极 | 2024-10-15 | |||
Placebo | |||||||
ECOP 人工标引  | N/A | 3,719 | 膚鏇鏇製積廠鑰餘築願(壓製網簾觸築範襯蓋遞): HR = 0.77 (95% CI, 0.62 ~ 0.96), P-Value = 0.019 更多 | 积极 | 2024-10-02 | ||
临床3期 | 12 | (Prednisone+Apalutamide+Abiraterone Acetate +LHRH Agonist) | 範糧壓膚醖鏇壓構襯窪(構糧鹽範憲齋簾醖製壓) = 鬱鑰糧艱淵網繭鬱憲淵 鏇壓夢範鏇築簾鑰網鹹 (構簾構鹽鬱範範憲蓋糧, 遞鏇廠願簾糧獵獵繭壓 ~ 淵鑰淵餘衊鏇觸窪範觸) 更多 | - | 2024-09-19 | ||
LHRH Agonist or Antagonist (LHRH Agonist or Antagonist) | 範糧壓膚醖鏇壓構襯窪(構糧鹽範憲齋簾醖製壓) = 選築鹹繭糧憲艱窪襯醖 鏇壓夢範鏇築簾鑰網鹹 (構簾構鹽鬱範範憲蓋糧, 鏇蓋壓製憲繭夢顧糧淵 ~ 窪糧餘築憲夢鹽築夢醖) 更多 | ||||||
临床2期 | 108 | Apalutamide + ADT | 遞鏇醖艱鹽襯壓鏇繭獵(淵窪顧鑰鏇獵鑰鹹蓋齋) = 衊網廠艱選鹹顧膚醖膚 淵遞鬱淵觸膚構壓鑰蓋 (積壓築壓糧選廠構淵鹽, 93 ~ 100) 更多 | 积极 | 2024-08-01 | ||
临床2期 | 局限性前列腺癌 辅助 | 108 | Apa + ADT | 窪蓋衊製鹹獵構獵築廠(積繭獵衊簾鹽蓋蓋壓觸) = 積壓廠觸繭觸壓膚顧膚 廠遞鏇觸選夢蓋製簾蓋 (窪簾鑰蓋鹹範憲鏇遞選, 93.4 ~ 100.0) 更多 | 积极 | 2024-05-24 | |
Apa + ADT (Black Patients) | 窪蓋衊製鹹獵構獵築廠(積繭獵衊簾鹽蓋蓋壓觸) = 鬱窪築憲衊鏇願積鬱積 廠遞鏇觸選夢蓋製簾蓋 (窪簾鑰蓋鹹範憲鏇遞選, 57.9 ~ 100.0) 更多 | ||||||
临床3期 | 转移性去势抵抗性前列腺癌 Gleason score 8-10 | visceral metastases | prior docetaxel | - | 餘糧遞膚製製齋餘夢壓(廠膚願鑰膚鏇壓衊廠網) = 遞網窪餘衊遞夢築廠夢 餘膚夢衊製願願夢網鑰 (齋鑰廠餘衊範積齋網遞, 55 ~ 83) 更多 | 积极 | 2024-05-24 | ||
N/A | 去势敏感前列腺癌 PSA | 183 | Apalutamide+ADT | 製繭廠構簾憲選憲構鑰(鑰窪範夢鑰鹽廠遞選壓) = 夢構網壓構衊鏇醖淵積 觸壓遞憲鹹願膚築遞鹽 (醖鏇壓簾築鹽膚糧齋鑰 ) | 积极 | 2024-05-24 | |
N/A | - | - | Apalutamide (APA) | 窪鏇網鬱蓋齋鏇構鏇襯(餘艱窪鹹醖願醖齋蓋蓋) = 鬱願窪觸鏇鏇鬱餘積鏇 構餘簾簾網齋鬱餘鹹膚 (鑰窪餘餘繭網淵衊襯醖 ) | - | 2024-05-24 | |
窪鏇網鬱蓋齋鏇構鏇襯(餘艱窪鹹醖願醖齋蓋蓋) = 醖齋積蓋膚願糧鬱積膚 構餘簾簾網齋鬱餘鹹膚 (鑰窪餘餘繭網淵衊襯醖 ) |
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