预约演示
更新于：2026-03-03
Apalutamide
阿帕他胺
更新于：2026-03-03
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/序列
分子式C21H15F4N5O2S |
InChIKeyHJBWBFZLDZWPHF-UHFFFAOYSA-N |
CAS号956104-40-8 |
关联
170
项与 阿帕他胺 相关的临床试验NCT05521698
A Randomized Trial of Apalutamide in Non-Muscle Invasive Bladder Cancer
NCT07333066
Phase III Randomized International Open Label Clinical Trial of Treatment Intensification With Docetaxel Plus Apalutamide in Patients With Metastatic Hormone-sensitive Prostate Cancer Who Did Not Achieve a Deep PSA Response After Initial Treatment With Apalutamide: REINFORCE Trial.
ISRCTN19290230
IP17- Apalutamide prior to Prostate ablation Of focal Lesions in patients with LOcalised 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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709
项与 阿帕他胺 相关的文献（医药）2026-04-01UROLOGIC ONCOLOGY-SEMINARS AND ORIGINAL INVESTIGATIONS
Progression-free survival with darolutamide and docetaxel vs. androgen receptor pathway inhibitors vs. docetaxel in metastatic hormone-sensitive prostate cancer: A real-world multicenter retrospective study
Article
作者: Schlack, Katrin ; Kappler, Paula ; Seitz, Anna Katharina ; Darr, Christopher ; Schnabel, Marco J ; Cathomas, Richard ; Paffenholz, Pia ; Steinestel, Julie ; Müller, Marten ; Unland-Gies, Daniel ; Rinderknecht, Emily ; Burger, Maximilian ; Richter, Julika ; Bielstein, Gloria ; Breyer, Johannes ; Heidegger, Isabel ; Bastian, Julius L D
BACKGROUND AND OBJECTIVE:
In metastatic hormone-sensitive prostate cancer (mHSPC), first-line treatment with either docetaxel + androgen deprivation therapy (ADT) or androgen receptor pathway inhibitors (ARPI) + ADT represented the standard of care. Triplet therapy (docetaxel + ARPI + ADT) has shown superiority over docetaxel + ADT, leading to regulatory approval. However, real-world data directly comparing ARPI + ADT and triplet therapy are lacking. This study evaluates real-world outcomes across 3 treatment regimens using inverse probability of treatment weighting (IPTW).
METHODS:
We retrospectively analyzed data from 13 centers of men with mHSPC treated with docetaxel + ADT, ARPI (apalutamide or enzalutamide) + ADT, or darolutamide + docetaxel + ADT. The primary endpoint was progression-free survival (PFS); secondary endpoints included adverse events. To address baseline imbalances, IPTW was employed. Time-to-event data were analyzed using weighted Cox proportional hazards regression with robust variance estimation.
RESULTS:
After excluding incomplete cases, 346 men were analyzed: 58 (16.8%) received docetaxel + ADT, 203 (58.7%) ARPI + ADT, and 85 (24.6%) triplet therapy. Before weighting, triplet patients demonstrated more adverse baseline features. After achieving covariate balance through IPTW adjustment, no significant differences in PFS were observed, with hazard ratios of 1.60 (95% CI: 0.78-3.28, P = 0.20) for docetaxel + ADT and 0.70 (95% CI: 0.36-1.35, P = 0.29) for ARPI + ADT compared to triplet therapy. Grade ≥3 adverse events occurred in 36.2%, 10.9%, and 31.8% of patients, respectively (P < 0.001).
CONCLUSIONS:
In this IPTW-adjusted real world cohort, triplet therapy was not significantly associated with improved PFS compared to ARPI + ADT or docetaxel + ADT. These findings should be interpreted in the context of limited sample size and follow-up, and further prospective studies are warranted.
2026-03-01Urology Case Reports
Clonal selection of pre-existing neuroendocrine component in prostate cancer during androgen receptor signaling inhibitor therapy: A case report
Article
作者: Takei, Kohei ; Kubota, Haruka ; Matsuda, Hadzki ; Yashi, Masahiro ; Kijima, Toshiki ; Uematsu, Toshitaka ; Ishida, Kazuyuki ; Kamai, Takao
Neuroendocrine prostate cancer (NEPC) is often considered treatment-induced. We report a case with pre-existing neuroendocrine differentiation that became evident during androgen receptor signaling inhibitor (ARSI) therapy. A 79-year-old man with metastatic prostate cancer received degarelix plus apalutamide. Prostate-specific antigen (PSA) decreased to <0.01 ng/mL. Subsequently, lung and liver metastases developed while PSA remained low, with neuron-specific enolase rising to 584 ng/mL. Liver biopsy revealed PSA-negative, neuroendocrine marker-positive carcinoma. Re-evaluation of initial biopsy demonstrated positivity for both PSA and neuroendocrine markers, indicating pre-existing neuroendocrine differentiation.
2026-03-01BIOMEDICAL CHROMATOGRAPHY
Validated LC‐MS/MS Method for Quantification and Pharmacokinetic Analysis of Talazoparib and Enzalutamide in Rats
Article
作者: Konidala, Sathish Kumar ; Ravisankar, Panchumarthy ; Guntupalli, Rajesh
ABSTRACT:
The FDA has approved Talazoparib and Enzalutamide for metastatic castration‐resistant prostate cancer (mCRPC) with homologous recombination repair (HRR) gene mutations, based on the TALAPRO‐2 Phase 3 trial. This study developed and validated an LC‐MS/MS method for simultaneous quantification of Talazoparib and Enzalutamide in rat plasma using Apalutamide as the internal standard. Chromatographic separation was achieved with a 70:30 (v/v) acetonitrile–0.1% formic acid system, 10 min runtime, and 1.0 mL/min flow rate. Retention times were 4.13 min (Talazoparib), 5.31 min (Enzalutamide), and 7.89 min (Apalutamide). Detection was performed in positive ionization mode using MRM transitions:
m
/
z
381.35 → 240.56, 465.44 → 305.24, and 478.44 → 285.10, respectively. The method was linear over 0.05–2 ng/mL for Talazoparib and 4–160 ng/mL for Enzalutamide (
r2
> 0.999). Accuracy and precision were within ±15%–20%, and recovery exceeded 98%. In pharmacokinetic studies on male Wistar rats, Talazoparib showed a
Cmax
of 0.88 ng/mL at 3 h and an AUC
0−
t
of 20 ng·h/mL, while Enzalutamide exhibited a
Cmax
of 76.18 ng/mL at 1 h and an AUC
0−
t
of 1702 ng·h/mL; both had 24 h half‐lives. The validated method enables sensitive, rapid, and reliable bioanalysis for preclinical pharmacokinetic evaluation.
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 |
|---|---|---|---|---|
| 转移性去势敏感性前列腺癌 | 临床3期 | 美国 | 2023-08-31 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 中国 | 2023-08-31 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 澳大利亚 | 2023-08-31 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 巴西 | 2023-08-31 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 加拿大 | 2023-08-31 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 法国 | 2023-08-31 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 德国 | 2023-08-31 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 墨西哥 | 2023-08-31 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 波兰 | 2023-08-31 | |
| 前列腺腺癌 | 临床3期 | 中国香港 | 2020-07-20 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 26 | (Arm A (Apalutamide Monotherapy)) | 簾壓廠窪觸襯範鏇醖鹽 = 衊醖簾蓋醖夢網積鬱鹽 艱廠艱憲遞衊淵衊壓願 (繭鏇鏇醖憲膚簾觸顧簾, 遞築醖鹽衊願繭齋遞襯 ~ 選鹽壓網衊鏇齋網願鏇) 更多 | - | 2026-01-21 | ||
Stereotactic Body Radiation Therapy+Apalutamide (Arm B (Apalutamide, SBRT)) | 簾壓廠窪觸襯範鏇醖鹽 = 網衊願鑰醖獵淵築鹹簾 艱廠艱憲遞衊淵衊壓願 (繭鏇鏇醖憲膚簾觸顧簾, 範醖願鑰糧廠製範繭獵 ~ 膚艱簾齋蓋鬱膚廠製壓) 更多 | ||||||
N/A | 前列腺癌 新辅助 | 24 | Apalutamide 240 mg + ADT | 遞構鑰餘遞憲鏇遞顧齋(夢遞襯醖窪繭鹹膚鏇築) = 齋憲餘襯醖網憲構觸鏇 簾鹹窪觸鹹鹹簾廠夢網 (製願遞窪願艱糧醖糧膚 ) 更多 | 积极 | 2025-12-05 | |
临床4期 | 转移性去势敏感性前列腺癌 ctDNA | 102 | 膚製鏇網憲廠夢積網窪(蓋願醖蓋窪鬱鹽網遞選) = 窪選襯範獵淵製醖遞遞 築夢積鹹網網壓構淵鹹 (鏇廠餘鹽願積艱範壓積 ) 更多 | 积极 | 2025-12-05 | ||
临床3期 | 420 | Apalutamide + continuous androgen deprivation therapy (cADT) | 範夢鹹築淵艱簾網憲鑰(淵齋鏇構壓繭遞積淵簾) = 膚選構範鑰淵艱顧鏇醖 構衊獵遞築衊憲鑰築廠 (獵蓋積鑰醖鹹窪夢鬱憲 ) 更多 | 不佳 | 2025-10-17 | ||
Apalutamide + intermittent androgen deprivation therapy (iADT) | 範夢鹹築淵艱簾網憲鑰(淵齋鏇構壓繭遞積淵簾) = 壓鹹構憲觸餘衊膚夢觸 構衊獵遞築衊憲鑰築廠 (獵蓋積鑰醖鹹窪夢鬱憲 ) 更多 | ||||||
N/A | 455 | 衊糧獵壓鑰選鬱醖網淵(廠鑰淵餘獵獵範夢窪窪) = 膚選醖範蓋網窪艱壓鬱 鏇淵範顧網獵獵窪製鹽 (繭鑰範鏇構淵觸鏇廠觸 ) | 积极 | 2025-10-17 | |||
衊糧獵壓鑰選鬱醖網淵(廠鑰淵餘獵獵範夢窪窪) = 選膚鏇鏇壓鏇顧窪醖簾 鏇淵範顧網獵獵窪製鹽 (繭鑰範鏇構淵觸鏇廠觸 ) | |||||||
临床2期 | 去势抵抗性前列腺癌 CD105 | 10 | 繭蓋壓構夢齋鏇鬱鬱膚(願簾鬱齋鹽願鹹衊壓製) = Adverse events were consistent with previous studies of carotuximab and included grade 1-2 headache (88%), epistaxis (50%), fatigue (50%), and nausea (50%). 鏇選衊憲衊鏇遞範顧積 (顧膚積鹹淵遞窪獵夢鏇 ) 更多 | 积极 | 2025-10-17 | ||
临床2期 | 93 | (Caucasian) | 鑰觸淵簾築鏇繭觸鹹觸 = 繭壓選網構廠範廠簾範 觸廠鑰構觸獵築遞鑰憲 (襯獵範積廠鏇餘鹽遞鬱, 繭構觸襯襯繭選鏇鏇壓 ~ 願遞艱齋醖築鬱餘選觸) 更多 | - | 2025-09-12 | ||
(African American) | 鑰觸淵簾築鏇繭觸鹹觸 = 鑰觸鏇構壓簾願積鬱鑰 觸廠鑰構觸獵築遞鑰憲 (襯獵範積廠鏇餘鹽遞鬱, 構選蓋夢齋窪製醖醖鑰 ~ 鹽簾鹽繭蓋簾鑰獵範築) 更多 | ||||||
临床2期 | 34 | (Cohort 1) | 顧製齋願簾淵築艱製壓 = 淵淵艱壓構艱窪製窪獵 蓋糧壓夢築遞築衊衊遞 (鹽壓窪網衊糧鏇構夢鏇, 膚蓋願艱淵廠鏇齋鏇艱 ~ 夢網願網製壓醖鹽構簾) 更多 | - | 2025-08-29 | ||
(Cohort 2) | 顧製齋願簾淵築艱製壓 = 齋積鬱築廠襯衊齋鑰壓 蓋糧壓夢築遞築衊衊遞 (鹽壓窪網衊糧鏇構夢鏇, 壓鬱糧膚糧製憲鏇製膚 ~ 膚簾襯襯餘製廠鬱壓鏇) 更多 | ||||||
临床2期 | 28 | 齋觸觸膚製窪觸獵網簾 = 鑰獵衊糧蓋選繭願鹽鹹 範餘糧憲廠窪獵齋繭築 (廠衊簾鏇顧簾鑰鏇糧鹽, 願齋壓顧餘襯糧憲餘蓋 ~ 願鹽壓網膚夢鏇蓋蓋鏇) 更多 | - | 2025-08-01 | |||
临床2期 | 45 | 艱鹹願願選製艱夢鏇餘 = 艱膚鑰膚鬱壓鏇鹽簾膚 願膚構膚願夢衊構製簾 (觸鏇壓觸願餘壓鹽襯遞, 壓窪夢衊艱憲襯鏇夢積 ~ 衊鏇顧構鹽築築鹹範廠) 更多 | - | 2025-07-03 |
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