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Lutetium (177Lu) zaregreptide dizuxetan
Tier C — Watch / tradeLutetium (177Lu) zaregreptide dizuxetan
Novartis
Originator
-
First approval
-
Expiry (public)
No sales data
Peak sales
In vivo diagnostic
Type
Targets：GRPR
Indications (approved)：Metastatic breast cancer, Breast cancer, Neoplasm, Prostate cancer, Neuroendocrine carcinoma, Solid tumour
Regional status
US
Phase II
2019-07-24
EU
Phase II
2019-07-24
China
Phase II
2024-08-14
Japan
-
Synthetic routes & intermediates5 routes
Originator routes × 0Optimised (non-patent) × 5Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OptimisedRoute 1Steps 6 · Total yield /
(I) 847759-1-a—(II) 847759-1-a—(III) 847759-1-a—(IV) 847759-1-a29022-11-5(V) 847759-1-a—(VI) 847759-1-a68858-20-8(VII) 847759-1-a—(VIII) 847759-1-a35661-39-3(IX) 847759-1-a—(X) 847759-1-a143824-78-6(XI) 847759-1-a, (XI) 847759-1-b—API · Lutetium (177Lu) zaregreptide dizuxetan
| Code | CAS No. | Intermediate |
|---|---|---|
| (I) 847759-1-a | - | (2S)-2-({[(9H-Fluoren-9-yl)methoxy]carbonyl}amino)-3-[1-(triphenylmethyl)-1H-imidazol-4-yl]propanoic acid |
| (II) 847759-1-a | - | Resin bound N-[[(9H-fluoren-9-yl)methoxy]carbonyl]-1-(triphenylmethyl)-L-histidine |
| (III) 847759-1-a | - | Resin bound 1-(triphenylmethyl)-L-histidine |
| (IV) 847759-1-a | 29022-11-5 | 2-(9H-Fluoren-9-ylmethoxycarbonylamino)acetic acid |
| (V) 847759-1-a | - | Resin bound glycyl-1-(triphenylmethyl)-L-histidine |
| (VI) 847759-1-a | 68858-20-8 | (2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-3-methylbutanoic acid |
| (VII) 847759-1-a | - | Resin bound L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (VIII) 847759-1-a | 35661-39-3 | (2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)propanoic acid |
| (IX) 847759-1-a | - | Resin bound L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (X) 847759-1-a | 143824-78-6 | (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)propanoic acid |
| (XI) 847759-1-a, (XI) 847759-1-b | - | Resin bound 1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
OptimisedRoute 2Steps 2 · Total yield /
(XI) 847759-1-a, (XI) 847759-1-b—(XII) 847759-1-b132327-80-1(XIII) 847759-1-b—(XIV) 847759-1-b86123-10-6(XV) 847759-1-b, (XV) 847759-1-c—API · Lutetium (177Lu) zaregreptide dizuxetan
| Code | CAS No. | Intermediate |
|---|---|---|
| (XI) 847759-1-a, (XI) 847759-1-b | - | Resin bound 1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XII) 847759-1-b | 132327-80-1 | (2S)-2-({[(9H-Fluoren-9-yl)methoxy]carbonyl}amino)-4-[(triphenylmethyl)carbamoyl]butanoic acid |
| (XIII) 847759-1-b | - | Resin bound N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XIV) 847759-1-b | 86123-10-6 | (2R)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-3-phenylpropanoic acid |
| (XV) 847759-1-b, (XV) 847759-1-c | - | Resin bound D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
OptimisedRoute 3Steps 2 · Total yield /
(XIX) 847759-1-c, (XIX) 847759-1-d—(XV) 847759-1-b, (XV) 847759-1-c—(XVI) 847759-1-c—(XVII) 847759-1-c—(XVIII) 847759-1-c137076-54-1API · Lutetium (177Lu) zaregreptide dizuxetan
| Code | CAS No. | Intermediate |
|---|---|---|
| (XIX) 847759-1-c, (XIX) 847759-1-d | - | Resin bound N-([2-oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XV) 847759-1-b, (XV) 847759-1-c | - | Resin bound D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XVI) 847759-1-c | - | (2-[4-[([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)methyl]anilino]-2-oxoethoxy)acetic acid |
| (XVII) 847759-1-c | - | Resin bound N-([2-[4-(aminomethyl)anilino]-2-oxoethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XVIII) 847759-1-c | 137076-54-1 | DOTA-Tris(t-Bu)ester |
OptimisedRoute 4Steps 2 · Total yield /
(XIX) 847759-1-c, (XIX) 847759-1-d—(XX) 847759-1-d—(XXI) 847759-1-d65530-92-9(XXII) 847759-1-d, (XXII) 847759-1-e—API · Lutetium (177Lu) zaregreptide dizuxetan
| Code | CAS No. | Intermediate |
|---|---|---|
| (XIX) 847759-1-c, (XIX) 847759-1-d | - | Resin bound N-([2-oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XX) 847759-1-d | - | N-([2-Oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XXI) 847759-1-d | 65530-92-9 | 1-Isobutyl-3-methylbutylamine |
| (XXII) 847759-1-d, (XXII) 847759-1-e | - | N-([2-Oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-N-(2,6-dimethylheptan-4-yl)-1-(triphenylmethyl)-L-histidinamide |
OptimisedRoute 5Steps 2 · Total yield /
(XXIII) 847759-1-e—(XXII) 847759-1-d, (XXII) 847759-1-e—API · Lutetium (177Lu) zaregreptide dizuxetan
| Code | CAS No. | Intermediate |
|---|---|---|
| (XXIII) 847759-1-e | - | 2-[4-[2-[[4-[[2-[2-[[(2R)-1-[[(2S)-5-Amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-(2,6-Dimethylheptan-4-ylamino)-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethoxy]acetyl]amino]phenyl]methylamino]-2-oxoethyl]-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid |
| (XXII) 847759-1-d, (XXII) 847759-1-e | - | N-([2-Oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-N-(2,6-dimethylheptan-4-yl)-1-(triphenylmethyl)-L-histidinamide |
Frequently asked questions
What are the approved indications of Lutetium (177Lu) zaregreptide dizuxetan?
Approved indications include: Metastatic breast cancer, Breast cancer, Neoplasm, Prostate cancer, Neuroendocrine carcinoma, Solid tumour.
When does the Lutetium (177Lu) zaregreptide dizuxetan patent expire?
No public expiry year is available for Lutetium (177Lu) zaregreptide dizuxetan yet; this page updates once verified.
How many synthesis routes are recorded for Lutetium (177Lu) zaregreptide dizuxetan?
5 synthesis routes are recorded; the shortest is 2 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Lutetium (177Lu) zaregreptide dizuxetan intermediates?
All intermediates in Lutetium (177Lu) zaregreptide dizuxetan routes have CAS profiles — you can submit an RFQ per CAS and it enters the Unibest matching pool.
How do I get a quote for Lutetium (177Lu) zaregreptide dizuxetan intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-10-07