Raltitrexed

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Raltitrexed is a drug catalogued in DrugCentral. It was first approved by the YEAR INTRODUCED in 1996. DrugCentral lists 15 molecular targets, including SLC19A1, FOLR1 and FOLR2.

• Molecular targets: SLC19A1, FOLR1, FOLR2 and SLC46A1 (15 listed in DrugCentral).
• ATC code: L01BA03 (Folic acid analogues).
• Molecular formula: C21H22N4O6S; molecular weight 458.50 g/mol.

Mechanism & targets

Molecular targets (15)

Target	Gene	Action	Activity
Folate transporter 1	SLC19A1	unknown	IC50 8.20
Folate receptor alpha	FOLR1	unknown	IC50 7.82
Folate receptor beta	FOLR2	unknown	IC50 7.66
Proton-coupled folate transporter	SLC46A1	unknown	IC50 7.00
Histone-lysine N-methyltransferase EHMT2	EHMT2	unknown	IC50 6.92
Thymidylate synthase	TYMS	unknown	IC50 6.59
Thymidylate synthase	Tyms	unknown	Ki 6.38
Bifunctional dihydrofolate reductase-thymidylate synthase	—	unknown	IC50 6.32
Thymidylate synthase	Tyms	unknown	IC50 6.05
Thymidylate synthase	thyA	unknown	IC50 5.28
Thymidylate synthase	thyA	unknown	IC50 5.24
Thymidylate synthase	thyA	unknown	IC50 5.10
Dihydrofolate reductase	DHFR	unknown	IC50 4.68
Dihydrofolate reductase	folA	unknown	IC50 4.64
Dihydrofolate reductase	dfrA17	unknown	IC50 4.64

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1996-01-01	YEAR INTRODUCED	—	—

ATC classification

ATC code	Therapeutic hierarchy
L01BA03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ANTIMETABOLITES › Folic acid analogues

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Myelosuppression	294.6
Bone marrow failure	111.4
Diarrhoea	98.8
Hepatic function abnormal	83.4
Neurotoxicity	75.1
Palmar-plantar erythrodysaesthesia syndrome	63.5
Disease progression	60.5
Neutropenia	52.3

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Raltitrexed is on its molecule page.

• Molecular formula: C₂₁H₂₂N₄O₆S
• Molecular weight: 458.50 g/mol
• CAS number: —
• InChIKey: IVTVGDXNLFLDRM-HNNXBMFYSA-N
• PubChem CID: 135400182

CN(CC1=CC2=C(C=C1)N=C(C)NC2=O)C1=CC=C(S1)C(=O)N[C@@H](CCC(O)=O)C(O)=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

How does Raltitrexed work?

Its molecular targets in DrugCentral include SLC19A1, FOLR1, FOLR2 and SLC46A1.

When was Raltitrexed first approved?

Raltitrexed was first approved by the YEAR INTRODUCED in 1996.

What is the chemical formula of Raltitrexed?

Raltitrexed has the molecular formula C21H22N4O6S and a molecular weight of 458.50 g/mol.

Sources

• DrugCentral drug card 2353 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL225071 — compound record and bioactivity
• PubChem CID 135400182 — chemical identifiers
• DrugBank DB00293 — drug record
• FDA UNII FCB9EGG971 — substance identity
• UniProt P41440 (SLC19A1) — target protein
• UniProt P15328 (FOLR1) — target protein
• UniProt P14207 (FOLR2) — target protein
• UniProt Q96NT5 (SLC46A1) — target protein
• UniProt Q96KQ7 (EHMT2) — target protein
• UniProt P04818 (TYMS) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.