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镥[177Lu] 特昔维匹肽
Tier B · 提前布局Lutetium (177Lu) vipivotide tetraxetan
Radiomedix Inc
原研
2022
首批上市
-
到期年（公开口径）
$1.99B ▲
峰值销售
偶联类药物
类型
靶点：PSMA
商品名：PLUVICTO、派威妥
适应症（已批准）：激素敏感性前列腺肿瘤、去势抵抗性前列腺肿瘤、前列腺癌
各地区研发/上市状态
美国
批准上市
2022-03-23
欧盟
批准上市
2022-12-09
中国
批准上市
2025-11-04
日本
批准上市
2025-09-19
合成路线与中间体7 routes
原研路线 × 0优化路线（非专利）× 7工艺路线 × 0
路线按「原研路线 → 优化路线 / 工艺路线（非专利）」排序。每条路线附本站自绘的路线流程图（中间体 → 原料药）与中间体表（编号 / CAS / 英文名），可直接用于供应商开发与询价。流程图由本站依据已授权的结构化数据自行渲染，未使用任何第三方路线图。
优化Route 1步骤 8 · 总收率 /
Lutetium (177Lu) vipivotide tetraxetan-00132677-01-3Lutetium (177Lu) vipivotide tetraxetan-00216874-06-9Lutetium (177Lu) vipivotide tetraxetan-003180839-17-2Lutetium (177Lu) vipivotide tetraxetan-004—Lutetium (177Lu) vipivotide tetraxetan-005—Lutetium (177Lu) vipivotide tetraxetan-006—Lutetium (177Lu) vipivotide tetraxetan-007—Lutetium (177Lu) vipivotide tetraxetan-008112883-43-9Lutetium (177Lu) vipivotide tetraxetan-009—Lutetium (177Lu) vipivotide tetraxetan-010—Lutetium (177Lu) vipivotide tetraxetan-011—Lutetium (177Lu) vipivotide tetraxetan-012137076-54-1Lutetium (177Lu) vipivotide tetraxetan-0131702967-37-0Lutetium (177Lu) vipivotide tetraxetan-014146982-27-6Lutetium (177Lu) vipivotide tetraxetan-015—API · 镥[177Lu] 特昔维匹肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Lutetium (177Lu) vipivotide tetraxetan-001 | 32677-01-3 | L-Glutamic acid di-tert-butyl ester hydrochloride |
| Lutetium (177Lu) vipivotide tetraxetan-002 | 16874-06-9 | L-Glutamic acid di(tert-butyl) ester |
| Lutetium (177Lu) vipivotide tetraxetan-003 | 180839-17-2 | Di-tert-butyl 2(S)-isocyanatopentanedioate |
| Lutetium (177Lu) vipivotide tetraxetan-004 | - | Di-tert-butyl N-[(trichloromethoxy)carbonyl]-L-glutamate |
| Lutetium (177Lu) vipivotide tetraxetan-005 | - | Resin bound H-Lys(Alloc)-OH |
| Lutetium (177Lu) vipivotide tetraxetan-006 | - | Resin bound (2S)-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)-6-([[(prop-2-en-1-yl)oxy]carbonyl]amino)hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-007 | - | Resin bound (2S)-6-amino-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-008 | 112883-43-9 | Fmoc-2-Nal-OH |
| Lutetium (177Lu) vipivotide tetraxetan-009 | - | Resin bound 6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-010 | - | Fmoc-tranexamic acid |
| Lutetium (177Lu) vipivotide tetraxetan-011 | - | Resin bound (2S)-6-[[(2S)-2-[[(1r,4S)-4-(aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-012 | 137076-54-1 | DOTA-Tris(t-Bu)ester |
| Lutetium (177Lu) vipivotide tetraxetan-013 | 1702967-37-0 | (3S,10S,14S)-3-[(Naphthalen-2-yl)methyl]-1,4,12-trioxo-1-[(1r,4S)-4-([2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)cyclohexyl]-2,5,11,13-tetraazahexadecane-10,14,16-tricarboxylic acid |
| Lutetium (177Lu) vipivotide tetraxetan-014 | 146982-27-6 | N6-[(Allyloxy)carbonyl]-N2-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-lysine |
| Lutetium (177Lu) vipivotide tetraxetan-015 | - | Resin bound N2-[[(9H-fluoren-9-yl)methoxy]carbonyl]-N6-[[(prop-2-en-1-yl)oxy]carbonyl]-L-lysine |
优化Route 2步骤 3 · 总收率 /
Lutetium (177Lu) vipivotide tetraxetan-011—Lutetium (177Lu) vipivotide tetraxetan-0131702967-37-0Lutetium (177Lu) vipivotide tetraxetan-0162253751-88-9Lutetium (177Lu) vipivotide tetraxetan-017170908-81-3Lutetium (177Lu) vipivotide tetraxetan-018—API · 镥[177Lu] 特昔维匹肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Lutetium (177Lu) vipivotide tetraxetan-011 | - | Resin bound (2S)-6-[[(2S)-2-[[(1r,4S)-4-(aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-013 | 1702967-37-0 | (3S,10S,14S)-3-[(Naphthalen-2-yl)methyl]-1,4,12-trioxo-1-[(1r,4S)-4-([2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)cyclohexyl]-2,5,11,13-tetraazahexadecane-10,14,16-tricarboxylic acid |
| Lutetium (177Lu) vipivotide tetraxetan-016 | 2253751-88-9 | (2S)-6-[[(2S)-2-[[(1r,4S)-4-(Aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-017 | 170908-81-3 | 2,2',2''-(10-[2-[(2,5-Dioxopyrrolidin-1-yl)oxy]-2-oxoethyl]-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid |
| Lutetium (177Lu) vipivotide tetraxetan-018 | - | (2S)-2-([[(2S)-1,5-Di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)-6-[[(2S)-3-(naphthalen-2-yl)-2-[[(1r,4S)-4-([2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)cyclohexane-1-carbonyl]amino]propanoyl]amino]hexanoic acid |
优化Route 3步骤 1 · 总收率 /
Lutetium (177Lu) vipivotide tetraxetan-0131702967-37-0API · 镥[177Lu] 特昔维匹肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Lutetium (177Lu) vipivotide tetraxetan-013 | 1702967-37-0 | (3S,10S,14S)-3-[(Naphthalen-2-yl)methyl]-1,4,12-trioxo-1-[(1r,4S)-4-([2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)cyclohexyl]-2,5,11,13-tetraazahexadecane-10,14,16-tricarboxylic acid |
优化Route 4步骤 5 · 总收率 176mg(PSMA-617 (Free))
Lutetium (177Lu) vipivotide tetraxetan-019530-62-1Lutetium (177Lu) vipivotide tetraxetan-00132677-01-3Lutetium (177Lu) vipivotide tetraxetan-0201025796-29-5Lutetium (177Lu) vipivotide tetraxetan-021—Lutetium (177Lu) vipivotide tetraxetan-022—Lutetium (177Lu) vipivotide tetraxetan-023—Lutetium (177Lu) vipivotide tetraxetan-008112883-43-9Lutetium (177Lu) vipivotide tetraxetan-009—Lutetium (177Lu) vipivotide tetraxetan-010—Lutetium (177Lu) vipivotide tetraxetan-011—API · 镥[177Lu] 特昔维匹肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Lutetium (177Lu) vipivotide tetraxetan-019 | 530-62-1 | 1,1-Bis(1H-imidazol-1-yl)methanone |
| Lutetium (177Lu) vipivotide tetraxetan-001 | 32677-01-3 | Di-tert-butyl L-glutamate hydrogen chloride |
| Lutetium (177Lu) vipivotide tetraxetan-020 | 1025796-29-5 | Di-tert-butyl N-(1H-imidazole-1-carbonyl)-L-glutamate |
| Lutetium (177Lu) vipivotide tetraxetan-021 | - | Resin bound Fmoc-L-Lys(ivDde) |
| Lutetium (177Lu) vipivotide tetraxetan-022 | - | Resin bound N6-[1-(4,4-dimethyl-2,6-dioxocyclohexylidene)-3-methylbutyl]-L-lysine |
| Lutetium (177Lu) vipivotide tetraxetan-023 | - | Resin bound (2S)-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)-6-[[1-(4,4-dimethyl-2,6-dioxocyclohexylidene)-3-methylbutyl]amino]hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-008 | 112883-43-9 | Fmoc-2-Nal-OH |
| Lutetium (177Lu) vipivotide tetraxetan-009 | - | Resin bound 6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-010 | - | (1r,4r)-4-[([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)methyl]cyclohexane-1-carboxylic acid |
| Lutetium (177Lu) vipivotide tetraxetan-011 | - | Resin bound (2S)-6-[[(2S)-2-[[(1r,4S)-4-(aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid |
优化Route 5步骤 1 · 总收率 286mg(Lutetium (177Lu) vipivotide tetraxetan-013)
Lutetium (177Lu) vipivotide tetraxetan-011—Lutetium (177Lu) vipivotide tetraxetan-012137076-54-1Lutetium (177Lu) vipivotide tetraxetan-0131702967-37-0API · 镥[177Lu] 特昔维匹肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Lutetium (177Lu) vipivotide tetraxetan-011 | - | Resin bound (2S)-6-[[(2S)-2-[[(1r,4S)-4-(aminomethyl)cyclohexane-1-carbonyl]amino]-3-(naphthalen-2-yl)propanoyl]amino]-2-([[(2S)-1,5-di-tert-butoxy-1,5-dioxopentan-2-yl]carbamoyl]amino)hexanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-012 | 137076-54-1 | DOTA-Tris(t-Bu)ester |
| Lutetium (177Lu) vipivotide tetraxetan-013 | 1702967-37-0 | (3S,10S,14S)-3-[(Naphthalen-2-yl)methyl]-1,4,12-trioxo-1-[(1r,4S)-4-([2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)cyclohexyl]-2,5,11,13-tetraazahexadecane-10,14,16-tricarboxylic acid |
优化Route 6步骤 5 · 总收率 176mg(PSMA-617 (Free))
Lutetium (177Lu) vipivotide tetraxetan-024—Lutetium (177Lu) vipivotide tetraxetan-019530-62-1Lutetium (177Lu) vipivotide tetraxetan-025—Lutetium (177Lu) vipivotide tetraxetan-026—Lutetium (177Lu) vipivotide tetraxetan-027—Lutetium (177Lu) vipivotide tetraxetan-028—Lutetium (177Lu) vipivotide tetraxetan-008112883-43-9Lutetium (177Lu) vipivotide tetraxetan-029—Lutetium (177Lu) vipivotide tetraxetan-010—Lutetium (177Lu) vipivotide tetraxetan-030—API · 镥[177Lu] 特昔维匹肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Lutetium (177Lu) vipivotide tetraxetan-024 | - | tert-Butyl N6-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-lysinate hydrogen chloride |
| Lutetium (177Lu) vipivotide tetraxetan-019 | 530-62-1 | Staab's reagent |
| Lutetium (177Lu) vipivotide tetraxetan-025 | - | tert-Butyl N6-[[(9H-fluoren-9-yl)methoxy]carbonyl]-N2-(1H-imidazole-1-carbonyl)-L-lysinate |
| Lutetium (177Lu) vipivotide tetraxetan-026 | - | Resin bound Fmoc-Glu(t-Bu) |
| Lutetium (177Lu) vipivotide tetraxetan-027 | - | Resin bound (2S)-2-amino-5-tert-butoxy-5-oxopentanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-028 | - | Resin bound (9S,13S)-9-(tert-butoxycarbonyl)-13-(3-tert-butoxy-3-oxopropyl)-1-(9H-fluoren-9-yl)-3,11-dioxo-2-oxa-4,10,12-triazatetradecan-14-oic acid |
| Lutetium (177Lu) vipivotide tetraxetan-008 | 112883-43-9 | Fmoc-2-Nal-OH |
| Lutetium (177Lu) vipivotide tetraxetan-029 | - | Resin bound (2S)-2-([[(2S)-6-[[(2S)-2-amino-3-(naphthalen-2-yl)propanoyl]amino]-1-tert-butoxy-1-oxohexan-2-yl]carbamoyl]amino)-5-tert-butoxy-5-oxopentanoic acid |
| Lutetium (177Lu) vipivotide tetraxetan-010 | - | Fmoc-tranexamic acid |
| Lutetium (177Lu) vipivotide tetraxetan-030 | - | Resin bound [(2S,6S,13S)-15-[(1r,4S)-4-(aminomethyl)cyclohexyl]-6-(tert-butoxycarbonyl)-2-(3-tert-butoxy-3-oxopropyl)-13-[(naphthalen-2-yl)methyl]-4,12,15-trioxo-3,5,11,14-tetraazapentadecanan-1-oyl]oxy |
优化Route 7步骤 1 · 总收率 286mg(Lutetium (177Lu) vipivotide tetraxetan-013)
Lutetium (177Lu) vipivotide tetraxetan-030—Lutetium (177Lu) vipivotide tetraxetan-012137076-54-1Lutetium (177Lu) vipivotide tetraxetan-0131702967-37-0API · 镥[177Lu] 特昔维匹肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Lutetium (177Lu) vipivotide tetraxetan-030 | - | Resin bound [(2S,6S,13S)-15-[(1r,4S)-4-(aminomethyl)cyclohexyl]-6-(tert-butoxycarbonyl)-2-(3-tert-butoxy-3-oxopropyl)-13-[(naphthalen-2-yl)methyl]-4,12,15-trioxo-3,5,11,14-tetraazapentadecanan-1-oyl]oxy |
| Lutetium (177Lu) vipivotide tetraxetan-012 | 137076-54-1 | DOTA-Tris(t-Bu)ester |
| Lutetium (177Lu) vipivotide tetraxetan-013 | 1702967-37-0 | (3S,10S,14S)-3-[(Naphthalen-2-yl)methyl]-1,4,12-trioxo-1-[(1r,4S)-4-([2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)cyclohexyl]-2,5,11,13-tetraazahexadecane-10,14,16-tricarboxylic acid |
常见问题（FAQ）
镥[177Lu] 特昔维匹肽的适应症有哪些？
已批准的适应症包括：激素敏感性前列腺肿瘤、去势抵抗性前列腺肿瘤、前列腺癌。
镥[177Lu] 特昔维匹肽的专利什么时候到期？
镥[177Lu] 特昔维匹肽的专利到期年暂无公开口径，本页会在数据管道核实后更新。
镥[177Lu] 特昔维匹肽有几条合成路线？
本站收录 7 条合成路线，最短路线 1 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
镥[177Lu] 特昔维匹肽的关键中间体在哪里可以采购？
镥[177Lu] 特昔维匹肽路线中的中间体均已建立 CAS 档案，可直接按 CAS 发起询价，需求会进入供应网络撮合池。
如何获取镥[177Lu] 特昔维匹肽中间体的报价？
在本页选择目标中间体的 CAS 进入档案页，或在询价页直接提交需求；CAS 会自动带入供需撮合流程，由供应网络反馈报价。
数据来源：多源数据交叉核实（仅结构化字段） · 2026-10-22