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Roxadustat · all drugs expiring in 2028 →

Fibrogen Inc
Originator
2018
First approval
2028
Expiry (public)
$0.33B ▲
Peak sales
化学药
Type

Targets：HIF-PHs

Brand：爱瑞卓

Indications (approved)：贫血

Regional status

US
临床三期
2012-11-05
EU
批准上市
2021-08-18
China
批准上市
2018-12-17
Japan
批准上市
2019-11-01

Synthetic routes & intermediates3 routes

Originator routes × 1Optimised (non-patent) × 2Process 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 9 · Total yield /
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
ROXA-00137951-15-8Available4-phenoxyphthalic acid
ROXA-00256-40-6Available2-aminoacetic acid
ROXA-003808115-49-3Available2-(1,3-dioxo-5-phenoxyisoindolin-2-yl)acetic acid
ROXA-004808115-50-6Availablemethyl 2-(1,3-dioxo-5-phenoxyisoindolin-2-yl)acetate
ROXA-005808115-51-7Availablebutyl 1,4-dihydroxy-7-phenoxyisoquinoline-3-carboxylate
ROXA-006808115-53-9Availablebutyl 1-bromo-4-hydroxy-7-phenoxyisoquinoline-3-carboxylate
ROXA-007808115-64-2Available1-bromo-4-hydroxy-7-phenoxyisoquinoline-3-carboxylic acid
ROXA-008808118-41-4Availablebenzyl 4-(benzyloxy)-1-methyl-7-phenoxyisoquinoline-3-carboxylate
ROXA-009808118-42-5Available4-(benzyloxy)-1-methyl-7-phenoxyisoquinoline-3-carboxylic acid
ROXA-0102462-31-9Availablebenzyl 2-aminoacetate hydrochloride
ROXA-011808118-43-6Availablebenzyl 2-(4-(benzyloxy)-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetate
OptimisedRoute 2Steps 10 · Total yield 0.21 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
ROXA-00137951-15-8Available4-phenoxyphthalic acid
ROXA-01231643-49-9Available4-nitrophthalonitrile
ROXA-01338791-62-7Available4-phenoxyphthalonitrile
ROXA-01421345-01-7Available5-phenoxyisobenzofuran-1,3-dione
ROXA-015105-34-0Availablemethyl 2-cyanoacetate
ROXA-0161421312-31-3Available2-(4-(methoxycarbonyl)oxazol-5-yl)-4-phenoxybenzoic acid
ROXA-0171421312-32-4Availablemethyl 4-hydroxy-1-oxo-7-phenoxy-1,2-dihydroisoquinoline-3-carboxylate
ROXA-0181421312-33-5Availablemethyl 1-chloro-4-hydroxy-7-phenoxyisoquinoline-3-carboxylate
ROXA-0191421312-34-6Availablemethyl 4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate
ROXA-0201421312-35-7Available4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylic acid
ROXA-0215680-79-5Availablemethyl glycinate hydrochloride
ROXA-0221421312-36-8Availablemethyl 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetate
OptimisedRoute 3Steps 9 · Total yield /
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
ROXA-00256-40-6Available2-aminoacetic acid
ROXA-0191421312-34-6Availablemethyl 4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate
ROXA-023108-95-2Availablephenol
ROXA-02464169-34-2Available5-bromoisobenzofuran-1(3H)-one
ROXA-02557830-14-5Available5-phenoxyisobenzofuran-1(3H)-one
ROXA-0261537180-07-6Available2-(chloromethyl)-4-phenoxybenzoyl chloride
ROXA-0271455091-04-9Availablemethyl 2-(chloromethyl)-4-phenoxybenzoate
ROXA-0282645-02-5Availablemethyl tosylglycinate
ROXA-0291455091-06-1Availablemethyl 2-((N-(2-methoxy-2-oxoethyl)-4-methylphenylsulfonamido)methyl)-4-phenoxybenzoate
ROXA-0301455091-10-7Availablemethyl 4-hydroxy-7-phenoxyisoquinoline-3-carboxylate
ROXA-03151-80-9AvailableN,N,N',N'-tetramethylmethanediamine
ROXA-0321509958-19-3Availablemethyl 1-((dimethylamino)methyl)-4-hydroxy-7-phenoxyisoquinoline-3-carboxylate
ROXA-0331509958-20-6Availablemethyl 1-(acetoxymethyl)-4-hydroxy-7-phenoxyisoquinoline-3-carboxylate

Frequently asked questions

What are the approved indications of Roxadustat?

Approved indications include: 贫血.

When does the Roxadustat patent expire?

Based on public sources, the Roxadustat patent expires in 2028.

How many synthesis routes are recorded for Roxadustat?

3 synthesis routes are recorded; the shortest is 9 steps with / total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Roxadustat intermediates?

33 intermediate CAS of Roxadustat are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.

How do I get a quote for Roxadustat 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) · 2026-09-24