Floxuridine

Summary

Floxuridine (CHEMBL917) is an approved small-molecule antineoplastic agent (ATC L01BC09); indicated across 19 conditions including neoplasm and colorectal adenocarcinoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01BC09
• Indications: 19 conditions
• Clinical trials: 51
• Chemistry: 246.19 Da · C9H11FN2O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL917
Name	Floxuridine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5790
ChEBI	CHEBI:60761
ATC	L01BC09
Molecular formula	C9H11FN2O5
Molecular weight	246.19
InChIKey	ODKNJVUHOIMIIZ-RRKCRQDMSA-N

SMILES: C1[C@@H]([C@H](O[C@H]1N2C=C(C(=O)NC2=O)F)CO)O

IUPAC name: 5-fluoro-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione

ChEBI definition: A pyrimidine 2’-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.

Pharmacological roles (ChEBI): antineoplastic agent, antiviral drug, radiosensitizing agent.

Other ChEBI roles (chemical / environmental): antimetabolite.

Also known as: F.u.d.r., Floxuridina, Floxuridine, Fluoruridine deoxyribose, FUDR, Fudr, NSC-27640, SID26748679, SID29215018, SID29215019, SID50104188, SID855946

Patent coverage: 26,061 distinct patent families (105,512 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Streptokinase A, Survival motor neuron protein, Prelamin-A/C, Thymidylate synthase.

Bioactivity

ChEMBL activities: 18 potent at pChembl ≥ 5 of 20 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P07607	9.4	IC50	0.4	nM	CHEMBL_ACT_6151513
P07607	9.4	IC50	0.4	nM	CHEMBL_ACT_6151518
P07607	9.22	IC50	0.6	nM	CHEMBL_ACT_6151508
P07607	9.22	IC50	0.6	nM	CHEMBL_ACT_6151523
P07607	9.15	IC50	0.7	nM	CHEMBL_ACT_6151528
P07607	9.15	IC50	0.7	nM	CHEMBL_ACT_6151533
LMNA	8.4	Potency	4	nM	CHEMBL_ACT_3651141
LMNA	8.35	Potency	4.5	nM	CHEMBL_ACT_3648718
P07607	8.1	IC50	7.9	nM	CHEMBL_ACT_338545
P07607	7.7	IC50	20	nM	CHEMBL_ACT_338548
P07607	7.37	IC50	43	nM	CHEMBL_ACT_272007
SMN1	6.75	Potency	177.8	nM	CHEMBL_ACT_3877997
P07607	6.58	IC50	260	nM	CHEMBL_ACT_338546
LMNA	6.45	Potency	354.8	nM	CHEMBL_ACT_3639198
P10520	6.16	EC50	689	nM	CHEMBL_ACT_4945449
SMN1	5.9	Potency	1259	nM	CHEMBL_ACT_3893482
P07607	5.27	IC50	5400	nM	CHEMBL_ACT_338547
P07607	5.14	IC50	7300	nM	CHEMBL_ACT_272010

Target pathways

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

Indications & clinical

Indications

3 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
neoplasm	4	MONDO:0005070	EFO:0000616
colorectal adenocarcinoma	3	MONDO:0005008	EFO:0000365
colorectal neoplasm	3	MONDO:0005335	EFO:0004142

12 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
hepatocellular carcinoma	2	MONDO:0007256	EFO:0000182
gastric adenocarcinoma	2	MONDO:0005036	EFO:0000503
cholangiocarcinoma	2	MONDO:0019087	EFO:0005221
intrahepatic cholangiocarcinoma	2	MONDO:0003210	EFO:1001961
carcinoid tumor	2	MONDO:0005369	EFO:0004243
gastric neoplasm	2	MONDO:0021085	MONDO:0001056
peritoneal neoplasm	2	MONDO:0006901	MONDO:0002087
ovarian cancer	2	MONDO:0008170	MONDO:0008170
gastrointestinal stromal tumor	2	MONDO:0011719	MONDO:0011719
rectal cancer	1	MONDO:0006519	EFO:1000657
fallopian tube neoplasm	1	MONDO:0021092	MONDO:0002158
colonic neoplasm	1	MONDO:0005401	MONDO:0021063

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

Clinical trials

Total trials: 51.

Phase distribution

Phase	Trials
PHASE2	31
PHASE1	9
PHASE3	8
PHASE2/PHASE3	1
PHASE1/PHASE2	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05863195	PHASE3	RECRUITING	Testing Pump Chemotherapy in Addition to Standard of Care Chemotherapy Versus Standard of Care Chemotherapy Alone for Patients With Unresectable Colorectal Liver Metastases: The PUMP Trial
NCT00002716	PHASE3	COMPLETED	Combination Chemotherapy in Treating Patients With Liver Metastases From Colorectal Cancer
NCT00020501	PHASE3	COMPLETED	Chemotherapy With or Without Isolated Hepatic Perfusion With Melphalan in Treating Patients With Colorectal Cancer That Has Spread to the Liver
NCT00268463	PHASE3	TERMINATED	Oxaliplatin and Capecitabine With or Without an Hepatic Arterial Infusion With Floxuridine in Treating Patients Who Are Undergoing Surgery and/or Ablation for Liver Metastases Due to Colorectal Cancer
NCT00643877	PHASE3	UNKNOWN	Trial of Preoperative Hepatic and Regional Arterial Chemotherapy (PHRAC) to Prevent Postoperative Liver Metastasis of Colorectal Cancer
NCT02402972	PHASE3	UNKNOWN	A Multi-center Randomized Controlled Trial of Intraportal Chemotherapy Combined With Adjuvant Chemotherapy (mFOLFOX6) for Stage II and III Colon Cancer
NCT03500874	PHASE3	TERMINATED	Adjuvant Systemic Chemotherapy With or Without HAI-FUDR in Patients With Resected CRLM
NCT03678428	PHASE3	TERMINATED	FUDR/Oxaliplatin HAI Plus Irinotecan vs. FOLFOXIRI Chemotherapy in Treating Initially Unresectable CRCLM
NCT04552093	PHASE2/PHASE3	UNKNOWN	Hepatic Arterial Infusion Pump Chemotherapy Combined With Systemic Chemotherapy (PUMP-IT)
NCT00492999	PHASE2	ACTIVE_NOT_RECRUITING	Hepatic Arterial Infusion With Floxuridine and Dexamethasone Combined With Combination Chemotherapy in Treating Patients With Colorectal Cancer That Has Spread to the Liver
NCT03856658	PHASE2	ACTIVE_NOT_RECRUITING	Hepatic Artery Infusional Floxuridine to Treat Pancreatic Cancer Liver Metastases
NCT04251715	PHASE2	ACTIVE_NOT_RECRUITING	mFOLFIRINOX Followed by Hepatic Arterial Infusion of Floxuridine and Dexamethasone With Systemic mFOLFIRI for Unresectable Liver-dominant Intrahepatic Cholangiocarcinoma
NCT04891289	PHASE2	RECRUITING	Gemcitabine and Oxaliplatin Chemotherapy With or Without a Floxuridine and Dexamethasone Pump in People With Cholangiocarcinoma That Cannot Be Removed With Surgery
NCT04898504	PHASE2	ACTIVE_NOT_RECRUITING	HAI-Floxuridine, or Liver-Tx, Combined With 2nd Line Chemotherapy Versus 2nd Line Chemotherapy Alone for Patients With Colorectal Liver Metastases and Heavy Tumour Burden.
NCT05286814	PHASE2	RECRUITING	PDS01ADC in Combination With Hepatic Artery Infusion Pump (HAIP) and Systemic Therapy for Subjects With Metastatic Colorectal Cancer, Intrahepatic Cholangiocarcinoma, or Metastatic Adrenocortical Carcinoma
NCT06313203	PHASE2	RECRUITING	HAI-Floxuridine, or SIRT, Combined With Gemox For Patients With Intra-Hepatic Cholangiocarcinoma Not Amenable to Resection (TOMCAT)
NCT00002783	PHASE2	COMPLETED	Combination Chemotherapy Before and After Surgery in Treating Patients With Stomach Cancer
NCT00002842	PHASE2	COMPLETED	Liver Resection and Floxuridine Plus Fluorouracil and Leucovorin in Treating Patients With Liver Metastases From Colorectal Cancer
NCT00003753	PHASE2	COMPLETED	Floxuridine, Dexamethasone, and Irinotecan After Surgery in Treating Patients With Liver Metastases From Colorectal Cancer
NCT00004103	PHASE2	COMPLETED	Combination Chemotherapy Followed by Surgery in Treating Patients With Stomach Cancer
NCT00004142	PHASE2	COMPLETED	Radiofrequency Ablation Followed By Hepatic Artery Chemotherapy in Treating Patients With Colorectal Cancer That Has Spread to the Liver
NCT00005049	PHASE2	COMPLETED	Combination Chemotherapy in Treating Patients With Stage III Ovarian Epithelial Cancer or Gastrointestinal Cancer
NCT00006038	PHASE2	COMPLETED	Combination Chemotherapy Followed by Surgery and Intraperitoneal Chemotherapy in Treating Patients With Locally Advanced Stomach Cancer
NCT00019760	PHASE2	COMPLETED	Isolated Hepatic Perfusion With Melphalan Followed By Chemotherapy in Treating Patients With Unresectable Colorectal Cancer That is Metastatic to the Liver
NCT00026234	PHASE2	COMPLETED	Hepatic Arterial Infusion Plus Chemotherapy in Treating Patients With Colorectal Cancer Metastatic to the Liver
NCT00063960	PHASE2	COMPLETED	Hepatic Arterial Infusion With Floxuridine and Systemic Irinotecan After Surgery in Treating Patients With Hepatic (Liver) Metastases From Colorectal Cancer
NCT00183911	PHASE2	COMPLETED	Study of 5-Fluorouracil and Leucovorin and Intra-abdominal Floxuridine Chemoradiation in Patients With Fully Resected Locally Advanced Gastric Adenocarcinoma
NCT00408551	PHASE2	UNKNOWN	Chemotherapy and Internal Radiation in Treating Patients With Colorectal Cancer That Has Spread to the Liver
NCT00410956	PHASE2	COMPLETED	Floxuridine and Dexamethasone as a Hepatic Arterial Infusion and Bevacizumab in Treating Patients With Primary Liver Cancer That Cannot be Removed by Surgery
NCT00448682	PHASE2	TERMINATED	Combination Chemotherapy as First-Line Therapy in Treating Patients With Stage IV Gastric Cancer That Cannot Be Removed By Surgery
NCT00448760	PHASE2	COMPLETED	Combination Chemotherapy in Treating Patients With Previously Untreated Stage II or Stage III Esophageal Cancer That Can Be Removed By Surgery
NCT00449163	PHASE2	TERMINATED	Combination Chemotherapy and Bevacizumab in Treating Patients With Stage IV Colorectal Cancer
NCT00587067	PHASE2	COMPLETED	A Phase II Study of Continuous Hepatic Arterial Infusion With Floxuridine (FUDR) and Dexamethasone (DEX) in Patients With Unresectable Primary Hepatic Malignancy
NCT00645710	PHASE1/PHASE2	COMPLETED	Hepatic Arterial Infusion of Floxuridine, Gemcitabine Hydrochloride, and Radiolabeled Monoclonal Antibody Therapy in Treating Liver Metastases in Patients With Metastatic Colorectal Cancer Previously Treated With Surgery
NCT00848783	PHASE2	TERMINATED	Irinotecan/Cisplatin, Potentially Curative Surgery With or Without Floxuridine, Followed by Capecitabine for Stomach and Gastro-esophageal Junction (GEJ) Cancers
NCT00858338	PHASE2	COMPLETED	Adjuvant Intraperitoneal Floxuridine Added to Chemoradiation for Fully Resected Advanced Stomach Cancer
NCT01862315	PHASE2	COMPLETED	Hepatic Arterial Infusion (HAI) With Floxuridine (FUDR) and Dexamethasone (Dex) Combined With Systemic Gemcitabine and Oxaliplatin in Patients With Unresectable Intrahepatic Cholangiocarcinoma (ICC)
NCT03069950	PHASE2	WITHDRAWN	Study of Chemotherapy With or Without Hepatic Arterial Infusion for Patients With Unresectable Metastatic Colorectal Cancer to the Liver
NCT03493061	PHASE2	COMPLETED	A Study of Systemic Chemotherapy With CPT-11 Plus HAI (FUDR+L-OHP) in Patients With Initially Unresectable CRCLM
NCT03693807	PHASE2	COMPLETED	A Study of the Use of the Medtronic Pump and Codman Catheter to Give Chemotherapy to Patients With Colorectal Carcinoma or Cholangiocarcinoma
NCT04668976	PHASE2	UNKNOWN	A Study of the Use of the Medtronic Pump and Codman Catheter to Give Chemotherapy to Patients With Colorectal Carcinoma or Cholangiocarcinoma
NCT00001576	PHASE1	COMPLETED	A Phase I Study of Isolated Hepatic Perfusion With Escalating Dose Melphalan Followed by Postoperative Hepatic Arterial Floxuridine and Leucovorin for Metastatic Unresectable Colorectal Cancers of the Liver
NCT00005860	PHASE1	COMPLETED	Oxaliplatin With Or Without Floxuridine and Leucovorin in Treating Patients With Metastatic Cancer of the Peritoneum
NCT00008294	PHASE1	COMPLETED	Combination Chemotherapy in Treating Patients With Unresectable Liver Metastases From Colorectal Cancer
NCT00059930	PHASE1	COMPLETED	Adjuvant Hepatic Arterial Infusion and Combination Chemotherapy in Treating Patients With Resectable Hepatic Metastases From Colorectal Cancer
NCT00695201	PHASE1	COMPLETED	Hepatic Arterial Infusion With Floxuridine and Dexamethasone in Combination With Intravenous Oxaliplatin Plus Irinotecan in Patients With Unresectable Hepatic Metastases From Colorectal Cancer
NCT01525069	PHASE1	TERMINATED	Hepatic Arterial Infusion in Treating Patients With Locally Advanced, Non-Metastatic Cholangiocarcinoma
NCT01749397	PHASE1	COMPLETED	Veliparib and Floxuridine in Treating Patients With Metastatic Epithelial Ovarian, Primary Peritoneal Cavity, or Fallopian Tube Cancer
NCT01938729	PHASE1	COMPLETED	Hepatic Arterial Infusion With Floxuridine and Dexamethasone in Combination With Gemcitabine as Adjuvant Treatment After Resection of Intrahepatic Cholangiocarcinoma
NCT03876574	PHASE1	COMPLETED	Hepatic Artery Infusion Pump for NPC Liver Metastases
NCT00522509	Not specified	UNKNOWN	Preoperative Hepatic Arterial Infusion Chemotherapy

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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