Arfolitixorin

Summary

Arfolitixorin (CHEMBL1234270) is a phase-3 clinical-stage small-molecule cofactor; indicated across 7 conditions including colorectal neoplasm and rectal cancer.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 7 conditions
• Clinical trials: 4
• Chemistry: 457.4 Da · C20H23N7O6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1234270
Name	Arfolitixorin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	135398645
ChEBI	CHEBI:1989
Molecular formula	C20H23N7O6
Molecular weight	457.4
InChIKey	QYNUQALWYRSVHF-OLZOCXBDSA-N

SMILES: C1[C@@H]2CN(CN2C3=C(N1)N=C(NC3=O)N)C4=CC=C(C=C4)C(=O)N[C@@H](CCC(=O)O)C(=O)O

IUPAC name: (2S)-2-[[4-[(6aR)-3-amino-1-oxo-2,5,6,6a,7,9-hexahydroimidazo[1,5-f]pteridin-8-yl]benzoyl]amino]pentanedioic acid

ChEBI definition: The (6R)-stereoisomer of 5,10-methylenetetrahydrofolic acid.

Pharmacological roles (ChEBI): cofactor.

Other ChEBI roles (chemical / environmental): Escherichia coli metabolite, mouse metabolite.

Also known as: 6r-mthf, Arfolitixorin, Arfolitixorina, Arfolitixorine, ISO-901, Modufolin, ARFOLITIXORIN

Patent coverage: 140 distinct patent families (457 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 455 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

7 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
colorectal neoplasm	3	MONDO:0005335	EFO:0004142
rectal cancer	1	MONDO:0006519	EFO:1000657
osteosarcoma	1	MONDO:0009807	EFO:0000637
colonic neoplasm	1	MONDO:0005401	EFO:0004288
neoplasm	1	MONDO:0005070	EFO:0000616

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE1/PHASE2	2
PHASE3	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03750786	PHASE3	COMPLETED	A Study to Compare the Efficacy of Arfolitixorin Versus Leucovorin in Combination With 5 Fluorouracil, Oxaliplatin, and Bevacizumab in Patients With Advanced Colorectal Cancer
NCT02244632	PHASE1/PHASE2	COMPLETED	Modufolin (Arfolitixorin) in Combination With 5-Fluorouracil Alone or Together With Oxaliplatin or Irinotecan in Colorectal Cancer
NCT04126655	PHASE1/PHASE2	UNKNOWN	Modelle 001, TS-inhibition in Colorectal Liver Metastases Comparing Arfolitixorin and Calciumfolinate
NCT03203564	PHASE1	COMPLETED	Study Evaluating ECG Effects, Safety, Tolerability and Pharmacokinetics of Single Doses of Modufolin (Arfolitixorin) in Healthy Volunteers Tetrahydrofolate in Healthy Male Volunteers

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).