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Fludarabine

drug
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Also known as FludarabinaFluradosaNSC-118218NSC-118218HSID855645SID144206348SID144206969SID170464764C0165064

Summary

Fludarabine (CHEMBL1568) is an approved small molecule targeting RRM1 and RRM2; indicated across 118 conditions including b-cell chronic lymphocytic leukemia and neoplasm of mature b-cells.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • Targets: 2 (RRM1, RRM2)
  • Indications: 118 conditions
  • Clinical trials: 1,165
  • Chemistry: 285.23 Da · C10H12FN5O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1568
NameFludarabine
TypeSmall molecule
Max phase3
FDA approvedyes
PubChem CID657237
Molecular formulaC10H12FN5O4
Molecular weight285.23
InChIKeyHBUBKKRHXORPQB-FJFJXFQQSA-N

SMILES: C1=NC2=C(N=C(N=C2N1[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)O)F)N

IUPAC name: (2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol

Also known as: Fludarabina, Fludarabine, Fluradosa, NSC-118218, NSC-118218H, fludarabine, SID855645, SID144206348, SID144206969, FLUDARABINE, SID170464764, C0165064

Patent coverage: 25,884 distinct patent families (101,629 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 101,427 (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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
RRM1ribonucleotide reductase catalytic subunit M1Inhibition6100% (common-essential)P23921
RRM2ribonucleotide reductase regulatory subunit M2Inhibition699.8% (common-essential)P31350

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Prelamin-A/C, Beta-lactamase, Adenosine receptor A2a, Adenosine receptor A1, Adenosine receptor A3, Hypoxia-inducible factor 1-alpha, 5’-nucleotidase.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P250998.23Ki5.9nMCHEMBL_ACT_1155200
P305437.55Ki28nMCHEMBL_ACT_1155201
HIF1A5.2Potency6310nMCHEMBL_ACT_4126755
HIF1A5.2Potency6310nMCHEMBL_ACT_4520166

Target pathways

Aggregated over 2 target gene(s): RRM1, RRM2.

Top Reactome pathways

3 total, by targets touching each:

PathwayTargetsGenes
Interconversion of nucleotide di- and triphosphates2RRM1, RRM2
G1/S-Specific Transcription1RRM2
Transcriptional Regulation by E2F61RRM2

Dominant GO biological processes

GO termTargets
DNA repair2
ribonucleoside diphosphate metabolic process2
deoxyribonucleotide biosynthetic process2
2’-deoxyribonucleotide biosynthetic process2
protein heterotetramerization2
positive regulation of G1/S transition of mitotic cell cycle2
DNA synthesis involved in DNA repair1
pyrimidine nucleobase metabolic process1
mitochondrial DNA replication1
male gonad development1
response to ionizing radiation1
positive regulation of G2/M transition of mitotic cell cycle1
cell proliferation in forebrain1
retina development in camera-type eye1
positive regulation of G0 to G1 transition1

Indications & clinical

Indications

118 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).

IndicationTrial phaseMONDOEFO
B-cell chronic lymphocytic leukemia3MONDO:0004948EFO:0000095
neoplasm of mature B-cells3MONDO:0004949EFO:0000096
myelodysplastic syndrome3MONDO:0018881EFO:0000198
acute lymphoblastic leukemia3MONDO:0004967EFO:0000220
acute myeloid leukemia3MONDO:0018874EFO:0000222
chronic myeloid leukemia3MONDO:0011996EFO:0000339
cutaneous melanoma3MONDO:0005012EFO:0000389
diffuse large B-cell lymphoma3MONDO:0018905EFO:0000403
leukemia3MONDO:0005059EFO:0000565
lymphoma3MONDO:0005062EFO:0000574
systemic sclerosis3MONDO:0005100EFO:0000717
melanoma3MONDO:0005105EFO:0000756
plasma cell myeloma3MONDO:0009693EFO:0001378
metastatic melanoma3MONDO:0005191EFO:0002617
non-Hodgkin lymphoma3MONDO:0018908EFO:0005952
aplastic anemia3MONDO:0015909EFO:0006927
mantle cell lymphoma3MONDO:0018876EFO:1001469
sickle cell disease3MONDO:0011382MONDO:0011382
follicular lymphoma3MONDO:0018906MONDO:0018906
hepatocellular carcinoma2MONDO:0007256EFO:0000182
Hodgkins lymphoma2MONDO:0004952EFO:0000183
MALT lymphoma2MONDO:0007650EFO:0000191
peripheral T-cell lymphoma, not otherwise specified2MONDO:0004964EFO:0000211
Burkitt lymphoma2MONDO:0007243EFO:0000309
clear cell renal carcinoma2MONDO:0005005EFO:0000349
Crohn disease2MONDO:0005011EFO:0000384
germ cell tumor2MONDO:0005040EFO:0000514
neoplasm2MONDO:0005070EFO:0000616
neuroblastoma2MONDO:0005072EFO:0000621
psoriasis2MONDO:0005083EFO:0000676
renal cell carcinoma2MONDO:0005086EFO:0000681
ovarian carcinoma2MONDO:0005140EFO:0001075
lymphoid neoplasm2MONDO:0005157EFO:0001642
myeloproliferative neoplasm2MONDO:0020076EFO:0002428
psoriatic arthritis2MONDO:0011849EFO:0003778
myelodysplastic syndrome with single lineage dysplasia2MONDO:0005272EFO:0003802
breast neoplasm2MONDO:0021100EFO:0003869
lymphoid leukemia2MONDO:0005402EFO:0004289
graft versus host disease2MONDO:0013730EFO:0004599
hematologic disorder2MONDO:0005570EFO:0005803
Waldenstrom macroglobulinemia2MONDO:0100280EFO:0009441
Langerhans cell histiocytosis2MONDO:0018310EFO:1000318
ocular melanoma2MONDO:0006325EFO:1000403
uveal melanoma2MONDO:0006486EFO:1000616
epidermolysis bullosa2MONDO:0006541EFO:1000690
acute erythroid leukemia2MONDO:0017858EFO:1001257
chronic myelomonocytic leukemia2MONDO:0020311EFO:1001779
thalassemia2MONDO:0000984EFO:1001996
inborn error of immunity2MONDO:0003778HP:0002721
fallopian tube neoplasm2MONDO:0021092MONDO:0002158
hematopoietic and lymphoid system neoplasm2MONDO:0002334MONDO:0002334
skin neoplasm2MONDO:0002531MONDO:0002898
multiple sclerosis2MONDO:0005301MONDO:0005301
ovarian cancer2MONDO:0008170MONDO:0008170
T-cell non-Hodgkin lymphoma2MONDO:0015760MONDO:0015760
chronic granulomatous disease2MONDO:0018305MONDO:0018305
autoimmune hemolytic anemia2MONDO:0020108MONDO:0018922
Fanconi anemia2MONDO:0019391MONDO:0019391
primary myelofibrosis2MONDO:0009692MONDO:0044903
beta thalassemia2MONDO:0019402Orphanet:848
B-cell acute lymphoblastic leukemia1MONDO:0004947EFO:0000094
Ewing sarcoma1MONDO:0012817EFO:0000174
head and neck squamous cell carcinoma1MONDO:0010150EFO:0000181
metastatic prostate carcinoma1MONDO:0004956EFO:0000196
T-cell acute lymphoblastic leukemia1MONDO:0004963EFO:0000209
glioblastoma1MONDO:0018177EFO:0000519
immune system disorder1MONDO:0005046EFO:0000540
lung adenocarcinoma1MONDO:0005061EFO:0000571
mesothelioma1MONDO:0005065EFO:0000588
osteosarcoma1MONDO:0009807EFO:0000637
prostate adenocarcinoma1MONDO:0005082EFO:0000673
rheumatoid arthritis1MONDO:0008383EFO:0000685
sarcoma1MONDO:0005089EFO:0000691
squamous cell lung carcinoma1MONDO:0005097EFO:0000708
cervical carcinoma1MONDO:0005131EFO:0001061
prostate carcinoma1MONDO:0005159EFO:0001663
non-small cell lung carcinoma1MONDO:0005233EFO:0003060
kidney neoplasm1MONDO:0021163EFO:0003865
anemia1MONDO:0002280EFO:0004272
lupus nephritis1MONDO:0005556EFO:0005761
vasculitis1MONDO:0018882EFO:0006803
CD4+/CD56+ hematodermic neoplasm1MONDO:0019467EFO:0010580
hepatoblastoma1MONDO:0018666EFO:1000292
juvenile myelomonocytic leukemia1MONDO:0011908EFO:1000309
paraganglioma1MONDO:0000448EFO:1000453
Sezary syndrome1MONDO:0017844EFO:1000785
mycosis fungoides1MONDO:0009691EFO:1001051
gliosarcoma1MONDO:0016681EFO:1001465
B-cell non-Hodgkin lymphoma1MONDO:0015759EFO:1001938
scleroderma1MONDO:0019340EFO:1001993
kidney failure1MONDO:0001106EFO:1002048
brain cancer1MONDO:0001657MONDO:0001657
kidney cancer1MONDO:0002367MONDO:0002367
adenocarcinoma1MONDO:0004970MONDO:0003219
myeloid leukemia1MONDO:0004643MONDO:0004643
pancreatic ductal adenocarcinoma1MONDO:0005184MONDO:0005184
systemic lupus erythematosus1MONDO:0007915MONDO:0007915
lung neoplasm1MONDO:0021117MONDO:0008903
severe combined immunodeficiency1MONDO:0015974MONDO:0015974
acute biphenotypic leukemia1MONDO:0020322MONDO:0019460
glioma1MONDO:0021042MONDO:0100342
nasopharyngeal carcinoma0MONDO:0015459MONDO:0015459
neuroepithelial neoplasm0MONDO:0021193MONDO:0021193

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

Clinical trials

Total trials: 1,165.

Phase distribution

PhaseTrials
PHASE1386
PHASE2364
PHASE1/PHASE2213
PHASE370
Not specified56
EARLY_PHASE139
PHASE2/PHASE319
PHASE418

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00198991PHASE4COMPLETEDGerman Multicenter Trial for Treatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Adults (07/2003)
NCT00199056PHASE4COMPLETEDGerman Multicenter Trial for Treatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Adults (06/99)
NCT00199147PHASE4UNKNOWNEfficacy of G-CSF-Priming in Elderly AML Patients
NCT00220311PHASE4COMPLETEDA Study to Confirm the Efficacy and Safety of Fludarabine Phosphate Administered in Untreated Chronic Lymphocytic Leukemia Patients With Anemia and/or Thrombocytopenia
NCT00361140PHASE4COMPLETEDBusulfan Safety/Efficacy as Conditioning Prior to Hematopoietic Cell Transplantation (HCT)
NCT00487448PHASE4COMPLETEDSMD_FLAG-IDA_98: FLAG-IDA in Induction Treatment of High Risk Myelodysplastic Syndromes or Secondary Acute Myeloblastic Leukemia
NCT00488709PHASE4COMPLETEDFludarabine, Cytarabine, Topotecan in Treating Patients With Relapsed or Refractory Acute Myeloid Leukemia
NCT01088724PHASE4COMPLETEDFludarabine, Cyclophosphamide, Doxorubicin and Rituximab for the Treatment of Post-transplant Lymphoproliferative Disease (PTLD)
NCT01271010PHASE4TERMINATEDA Study of Rituximab in Combination With Fludarabine and Cyclophosphamide in Participants With Chronic Lymphocytic Leukemia and Favorable Somatic Status
NCT01283386PHASE4TERMINATEDA Study to Compare Mabthera (Rituximab), Fludarabine and Cyclophosphamide to Mabthera and Chlorambucil in Participants With Chronic Lymphocytic Leukemia and Unfavorable Somatic Status
NCT02024308PHASE4UNKNOWNAML1-ETO Acute Myeloid Leukemia With Fludarabine and Cytarabine Chemotherapy
NCT02784561PHASE4UNKNOWNStudy of Busulfan and FLAG Conditioning Regimen for Allogeneic Peripheral Blood Stem Cell Transplantation
NCT02894645PHASE4UNKNOWNMalaysia-Singapore Acute Lymphoblastic Leukemia 2010 Study
NCT02926586PHASE4COMPLETEDFludarabine and Cytarabine Versus High-dose Cytarabine for CBF-AML
NCT03171831PHASE4UNKNOWNHaploidentical Hematopoietic Stem Cell Transplantation for Patients With Thalassemia Major
NCT04009525PHASE4COMPLETEDHematopoietic Stem Cell Transplantation for Patients With Thalassemia Major: A Multicenter, Prospective Clinical Study
NCT05108805PHASE4COMPLETEDChimeric Antigen Receptor (CAR) T Cell Therapy With YESCARTA in the Outpatient Setting
NCT05379569PHASE4UNKNOWNComparative Study of BFC and BuCy Conditioning Regimen for Allo-PBSCT in Acute B-cell ALL
NCT01949129PHASE2/PHASE3RECRUITINGAllogeneic Stem Cell Transplantation for Children and Adolescents With Acute Lymphoblastic Leukaemia
NCT02724163PHASE3RECRUITINGInternational Randomised Phase III Clinical Trial in Children With Acute Myeloid Leukaemia
NCT03182244PHASE3ACTIVE_NOT_RECRUITINGA Study of ASP2215 Versus Salvage Chemotherapy In Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) With FMS-like Tyrosine Kinase 3 (FLT3) Mutation
NCT03480360PHASE3ACTIVE_NOT_RECRUITINGHaploidentical Allogeneic Peripheral Blood Transplantation: Examining Checkpoint Immune Regulators’ Expression
NCT03937544PHASE2/PHASE3RECRUITINGIntravenous Autologous CD19 CAR-T Cells for R/R B-ALL
NCT04217278PHASE2/PHASE3ACTIVE_NOT_RECRUITINGA Trial of Treatments to Assess the Effects on Outcome of Adults With AML and MDS Undergoing Allogeneic SCT
NCT04923893PHASE3ACTIVE_NOT_RECRUITINGA Study of Bortezomib, Lenalidomide and Dexamethasone (VRd) Followed by Cilta-cel, a CAR-T Therapy Directed Against BCMA Versus VRd Followed by Lenalidomide and Dexamethasone (Rd) Therapy in Participants With Newly Diagnosed Multiple Myeloma for Whom ASCT is Not Planned as Initial Therapy
NCT05183035PHASE3RECRUITINGVenetoclax in Children With Relapsed Acute Myeloid Leukemia (AML)
NCT05257083PHASE3ACTIVE_NOT_RECRUITINGA Study of Daratumumab, Bortezomib, Lenalidomide and Dexamethasone (DVRd) Followed by Ciltacabtagene Autoleucel Versus Daratumumab, Bortezomib, Lenalidomide and Dexamethasone (DVRd) Followed by Autologous Stem Cell Transplant (ASCT) in Participants With Newly Diagnosed Multiple Myeloma
NCT05371093PHASE3ACTIVE_NOT_RECRUITINGStudy of Axicabtagene Ciloleucel Versus Standard of Care Therapy in Participants With Relapsed/Refractory Follicular Lymphoma
NCT05457556PHASE3ACTIVE_NOT_RECRUITINGMismatched Related Donor Versus Matched Unrelated Donor Stem Cell Transplantation for Children, Adolescents, and Young Adults With Acute Leukemia or Myelodysplastic Syndrome
NCT05600426PHASE3ACTIVE_NOT_RECRUITINGA Trial Comparing Unrelated Donor BMT With IST for Pediatric and Young Adult Patients With Severe Aplastic Anemia (TransIT, BMT CTN 2202)
NCT05605899PHASE3ACTIVE_NOT_RECRUITINGStudy to Compare Axicabtagene Ciloleucel With Standard of Care Therapy as First-line Treatment in Participants With High-risk Large B-cell Lymphoma
NCT05624554PHASE3ACTIVE_NOT_RECRUITINGA Study of Nemtabrutinib vs Chemoimmunotherapy for Participants With Previously Untreated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) Without TP53 Aberrations (MK-1026-008, BELLWAVE-008)
NCT05674539PHASE3ENROLLING_BY_INVITATIONReduced Intensity Conditioning Regimens for Acute Myeloid Leukemia and Myelodysplastic Syndrome
NCT05991908PHASE3RECRUITINGRandomized Study of Conditioning of Fludarabine Combined With Single or Dual Alkylating Agents in Myeloid Malignancies
NCT06045806PHASE3ACTIVE_NOT_RECRUITINGA Study to Compare the Efficacy and Safety of Idecabtagene Vicleucel With Lenalidomide Maintenance Therapy Versus Lenalidomide Maintenance Therapy Alone in Adult Participants With Newly Diagnosed Multiple Myeloma Who Have Suboptimal Response After Autologous Stem Cell Transplantation
NCT06297772PHASE3NOT_YET_RECRUITINGCompare the Efficacy and Safety of Dec-FB4 and FB4 as Conditioning Regimen for AML-MR
NCT06319456PHASE3RECRUITINGA Global Study of Lisaftoclax (APG-2575) Combined With Acalabrutinib Versus Immunochemotherapy for Newly Diagnosed CLL/SLL.
NCT06413498PHASE3RECRUITINGA Study Comparing Anitocabtagene Autoleucel to Standard of Care Therapy in Participants With Relapsed/ Refractory Multiple Myeloma
NCT06613035PHASE3NOT_YET_RECRUITINGTwice-per-weekSelinexor, 2 Days Melphalan
NCT06615479PHASE3RECRUITINGA Study to Compare the Efficacy and Safety of BMS-986393 Versus Standard Regimens in Adult Participants With Relapsed or Refractory and Lenalidomide-exposed Multiple Myeloma (QUINTESSENTIAL-2)

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

4 molecules share ≥1 primary target. Top 4 by shared-target count:

MoleculeSourceStatusShared targets
TRIAPINEChEMBLPhase 3RRM1, RRM2
ClofarabinePubChemApprovedRRM1, RRM2
GemcitabinePubChemApprovedRRM1, RRM2
HydroxyureaPubChemApprovedRRM1, RRM2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot