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Linsitinib

Tier C — Watch / trade

Linsitinib

Astellas Pharma Inc.
Originator
-
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type

Targets:IGF1R, INSR

Indications (approved):甲状腺疾病, 甲状腺相关性眼病, 慢性淋巴细胞性甲状腺炎, 突眼症, Multiple myeloma, 唇肿瘤, 基底鳞状细胞癌, 口腔癌

Regional status

US
Phase III
2009-12-01
EU
Phase III
2009-12-01
China
Discontinued
2010-11-11
Japan
-

Synthetic routes & intermediates2 routes

Originator routes × 1Optimised (non-patent) × 1Process 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.

OriginatorRoute 1Steps 3 · Total yield 15.6 kg (Linsitinib)
LINSI-001936901-73-4LINSI-002936901-74-5LINSI-003936901-75-6LINSI-004867164-54-3Linsitinib867160-71-2API · Linsitinib
CodeCAS No.Intermediate
LINSI-001936901-73-43-(1-bromo-8-chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutan-1-one
LINSI-002936901-74-5(1s,3s)-3-(1-bromo-8-chloroimidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol
LINSI-003936901-75-6(1s,3s)-3-(8-amino-1-bromoimidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol
LINSI-004867164-54-32-phenyl-7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinoline
Linsitinib867160-71-2(1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol
OptimisedRoute 2Steps 11 · Total yield /
LINSI-005612-60-2LINSI-006591-51-5LINSI-00727356-39-4LINSI-008867162-43-4LINSI-00914508-49-7LINSI-010867162-41-2LINSI-01185-41-6LINSI-012867162-39-8LINSI-013867162-37-6LINSI-01415760-36-8LINSI-015867163-52-8LINSI-016867163-50-6LINSI-017867163-54-0LINSI-018867165-62-6LINSI-019867163-02-8API · Linsitinib
CodeCAS No.Intermediate
LINSI-005612-60-27-methylquinoline
LINSI-006591-51-5phenyllithium
LINSI-00727356-39-47-methyl-2-phenylquinoline
LINSI-008867162-43-42-phenylquinoline-7-carbaldehyde
LINSI-00914508-49-72-chloropyrazine
LINSI-010867162-41-2(3-chloropyrazin-2-yl)(2-phenylquinolin-7-yl)methanol
LINSI-01185-41-6isoindoline-1,3-dione
LINSI-012867162-39-82-((3-chloropyrazin-2-yl)(2-phenylquinolin-7-yl)methyl)isoindoline-1,3-dione
LINSI-013867162-37-6(3-chloropyrazin-2-yl)(2-phenylquinolin-7-yl)methanamine
LINSI-01415760-36-83-methylenecyclobutane-1-carboxylic acid
LINSI-015867163-52-8N-((3-chloropyrazin-2-yl)(2-phenylquinolin-7-yl)methyl)-3-methylenecyclobutane-1-carboxamide
LINSI-016867163-50-67-(8-chloro-3-(3-methylenecyclobutyl)imidazo[1,5-a]pyrazin-1-yl)-2-phenylquinoline
LINSI-017867163-54-03-(8-chloro-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-(hydroxymethyl)cyclobutan-1-ol
LINSI-018867165-62-63-(8-chloro-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)cyclobutan-1-one
LINSI-019867163-02-8(1s,3s)-3-(8-chloro-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol

Frequently asked questions

What are the approved indications of Linsitinib?

Approved indications include: 甲状腺疾病, 甲状腺相关性眼病, 慢性淋巴细胞性甲状腺炎, 突眼症, Multiple myeloma, 唇肿瘤, 基底鳞状细胞癌, 口腔癌.

When does the Linsitinib patent expire?

No public expiry year is available for Linsitinib yet; this page updates once verified.

How many synthesis routes are recorded for Linsitinib?

2 synthesis routes are recorded; the shortest is 3 steps with 15.6 kg (Linsitinib) total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Linsitinib intermediates?

All intermediates in Linsitinib 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 Linsitinib 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) · 2026-10-21