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Table S1. Clinical trials implicating galectins as biomarkers (1).

STA EN CLINICAL STATU BIOMARKE TUMOR PHAS RESULT RT D TRIAL TITLE TARGETS S RS TYPES ES S DAT DA NUMBERS E TE Stoppe Pidilizumab in Treating d Patients With Stage III-IV Sep Jan NCT025301 Termin Gal-1 Lympho Phase without Diffuse Large B-Cell PD-1 201 20 25 ated Biomarker ma 2 public Following First 5 17 explana Remission tion. Breast Cancer and Se Not Oct NCT026055 Cardiotoxicity Induced by Recruit Radiothe Gal-3 Breast p Applic 201 12 RadioTherapy: the BACCARAT ing rapy Biomarker Cancer 20 able 5 Study 20 Pilot Study of Biomarkers and Jun Jul Cardiac MRI as Early NCT024944 Termin Radiothe Breast e y Indicators of Cardiac Exposure biomarker 53 ated rapy Cancer 201 20 Following Breast 5 17 Radiotherapy Biomarkers and Cardiac MRI Unkno July NCT024962 as Early Indicators of Cardiac Radiothe Gal-3 Breast wn 201 60 Exposure Following Breast rapy Biomarker Cancer status 5 Radiotherapy Early Detection of Ma Breast Not Sep NCT032973 Cardiovascular Changes After Recruit Radiothe Gal-3 y Cancer Applic 201 46 Radiotherapy for Breast ing rapy Biomarker 20 Female able 7 Cancer 21 Pharmacologic Reversal of Ventricular Remodeling in Active, De Childhood Cancer Survivors at May NCT013479 not Gal-3 Cancer Phase c Risk for Congestive Heart multiple 201 70 recruiti Biomarker Survivor 2 20 Failure (PREVENT-CHF): A 2 ng 20 Phase IIB Randomized Placebo-Controlled Trial Validation of Colon Colon Apr Oct NCT015116 Biomarkers for the Early Compl Gal-3 Cancer|R il - 201 53 Detection of Colorectal eted Biomarker ectal 20 1 Adenocarcinoma Cancer 19 A New Agent GM-CT-01 in Combination With 5-FU, Oct NCT003887 Withdr Gal-3 Colorect Phase Avastin and Leucovorin in Galectins 200 00 awn Biomarker al Cancer 2 Subjects With Colorectal 6 Cancer Malignan Apri Carvedilol in Preventing Heart NCT027175 Recruit Beta- Gal-3 t Phase l Failure in Childhood Cancer 07 ing blockers Biomarker Neoplas 2 201 Survivors m 6

Biomolecules 2020, 10, 750; doi:10.3390/biom10050750 www.mdpi.com/journal/biomolecules Biomolecules 2020, 10, 750 2 of 9

Table S2. Clinical trials implicating galectins as biomarkers (2).

STA EN CLINICAL STATU TARGET BIOMARK TUMOR PHAS RESUL RT D TRIAL TITLE S S ERS TYPES ES TS DA DA NUMBERS TE TE Galectin Inhibitor (GR-MD- Metasta Ma Nov NCT02117 02) and in Compl Gal-3 tic Phase y PD-1 201 362 Patients With Metastatic eted Biomarker Melano 1 201 8 Melanoma ma 4 Predicting Prognosis and Recurrence of Thyroid Active Aug July Gal-3 NCT03488 Cancer Via New Biomarkers, , not Gal-3 Thyroid 3, 31, Pronosti 134 Urinary Exosomal recruit Biomarker Cancer 201 202 c Thyroglobulin and Galectin- ing 8 3 3 and With or Without Phase Jan PD-1 Biomarker NCT01896 Ipilimumab in Treating Recrui Lympho 1| 24, +CTLA-4 s (Gal- 999 Patients With Relapsed or ting ma Phase 201 +CD30 1+Tim-3) Refractory Hodgkin 2 4 Lymphoma HDM201 in Combination With MBG453 or Jun Apr in Patients With e NCT03940 Recrui Tim-3 Phase 22, Acute Myeloid P53 AML 24, 352 ting Biomarker 1 202 (AML) or High-risk 201 1 Myelodysplastic Syndrome 9 (MDS) Neoadjuvant Ma Active (Pbr)/Nab- PD-1 + r Sep NCT03289 , not Tim-3 Breast Phase Followed by Chemot 23, 202 819 recruit Biomarker Cancer 2 Pbr//Cyclophosph h 201 0 ing amide in TNBC 8 Breast Pilot Study of Stereotactic Neoplas Ablation for Oligometastatic Sep Apr NCT02303 Compl Tim-3 ms|Bon Phase Breast Neoplasia in PD-1 201 201 366 eted Biomarker e 1 Combination With the Anti- 5 7 Neoplas PD-1 Antibody MK-3475 ms Nov OMega-3 Fatty Acid for the Sep NCT03661 Recrui Metabol Tim-3 Colon Phase 30, Immune Modulation of 202 047 ting ism Biomarker Cancer 2 201 Colon Cancer 3 9 Oct Colorect July NCT04001 Anti-PD-1 +/- RT for MSI-H Recrui Tim-3 Phase 10, PD-1 al 202 101 Solid Tumors ting Biomarker 2 201 Cancer 1 9 Gastroin Phase Feb Aug PDR001 Plus for NCT03609 Recrui Tim-3 testinal 1| 14, 30, Metastatic or Unresectable PD-1 424 ting Biomarker Stromal Phase 201 202 GIST Tumors 2 9 0 Biomolecules 2020, 10, 750 3 of 9

Table S3. Clinical trials implicating galectins as biomarkers (3).

STA EN CLINICAL STATU TARGET BIOMARK TUMOR PHAS RESUL RT D TRIAL TITLE S S ERS TYPES ES TS DA DA NUMBERS TE TE Trial of Anti-Tim-3 in Glioblas Feb Fe NCT03961 Combination With Anti-PD- Recrui Tim-3 toma Phase 18, b PD-1 971 1 and SRS in Recurrent ting Biomarker Multifor 1 202 20 GBM me 0 24 Ap Study of PDR001 and/or Oct r NCT03066 MBG453 in Combination Recrui Tim-3 Leukemi Phase 29, PD-1 1, 648 With in Patients ting Biomarker a 1 201 20 With AML or High Risk MDS 0 21 TSR-022 (Anti-TIM-3 No Oc NCT03680 Antibody) and TSR-042 Recrui Tim-3 Liver Phase v 4, t - 508 (Anti-PD-1 Antibody) in ting Biomarker Cancer 2 201 20 Patients With Liver Cancer 9 23 Jun Expression of the Inhibitory Fe Not e NCT03549 Receptors on Lymphocytes Compl Tim-3 Lung b Surgery Appli 14, 546 T Cells After Lung Cancer eted Biomarker Cancer 20 cable 201 Surgery. 19 8 De Study of Anti-telomerase T Unkno Not Dec NCT02846 Tim-3 Lung c CD4 Immunity in Metastatic wn - Appli 201 103 Biomarker Cancer 20 Lung Cancer status cable 5 19 Ma Sym023 (Anti-TIM-3) in Active Se y NCT03489 Patients With Advanced , not Tim-3 Lympho Phase p - 30, 343 Solid Tumor Malignancies recruit Biomarker ma 1 20 201 or ing 20 8 Sym021 Monotherapy and in Combination With Dec No NCT03311 Sym022 or Sym023 in Recrui Tim-3 Lympho Phase 7, v PD-1 412 Patients With Advanced ting Biomarker ma 1 201 20 Solid Tumor Malignancies 7 20 or Lymphomas PSCA-CAR T Cells in Ma Fe Treating Patients With y NCT03873 Recrui Tim-3 Phase b PSCA+ Metastatic CART mCRPC 23, 805 ting Biomarker 1 20 Castration Resistant 201 21 Prostate Cancer 9 Fecal Microbial Ma De Transplantation in Fecal + rch NCT03772 Recrui Tim-3 Melano Phase c Combination With Immuno 27, 899 ting Biomarker ma 1 20 Immunotherapy in th 201 23 Melanoma Patients (MIMic) 9 Pembrolizumab TX-naive Jun Ju Distant Mets Melanoma NCT03089 Recrui Tim-3 Melano Phase e 1, ne and Use of AMT (PET) at PD-1 606 ting Biomarker ma 2 201 20 Baseline as Imaging 7 22 Biomarker Biomolecules 2020, 10, 750 4 of 9

Table S4. Clinical trials implicating galectins as biomarkers (4).

STA EN CLINICAL STATU TARGET BIOMARK TUMOR PHAS RESUL RT D TRIAL TITLE S S ERS TYPES ES TS DA DA NUMBERS TE TE Feb Trial of Anti-Tim-3 in Glioblas Fe r NCT03961 Combination With Anti-PD- Recrui Tim-3 toma Phase b PD-1 18, 971 1 and SRS in Recurrent ting Biomarker Multifor 1 20 202 GBM me 24 0 Ap Study of PDR001 and/or Oct r NCT03066 MBG453 in Combination Recrui Tim-3 Leukemi Phase 29, PD-1 1, 648 With Decitabine in Patients ting Biomarker a 1 201 20 With AML or High Risk MDS 0 21 TSR-022 (Anti-TIM-3 No Oc NCT03680 Antibody) and TSR-042 Recrui Tim-3 Liver Phase v 4, t - 508 (Anti-PD-1 Antibody) in ting Biomarker Cancer 2 201 20 Patients With Liver Cancer 9 23 Jun Expression of the Inhibitory Fe Not e NCT03549 Receptors on Lymphocytes Compl Tim-3 Lung b Surgery Appli 14, 546 T Cells After Lung Cancer eted Biomarker Cancer 20 cable 201 Surgery. 19 8 De Study of Anti-telomerase T Unkno Not Dec NCT02846 Tim-3 Lung c CD4 Immunity in Metastatic wn - Appli 201 103 Biomarker Cancer 20 Lung Cancer status cable 5 19 Ma Sym023 (Anti-TIM-3) in Active Se y NCT03489 Patients With Advanced , not Tim-3 Lympho Phase p - 30, 343 Solid Tumor Malignancies recruit Biomarker ma 1 20 201 or Lymphomas ing 20 8 Sym021 Monotherapy and in Combination With Dec No NCT03311 Sym022 or Sym023 in Recrui Tim-3 Lympho Phase 7, v PD-1 412 Patients With Advanced ting Biomarker ma 1 201 20 Solid Tumor Malignancies 7 20 or Lymphomas Ma PSCA-CAR T Cells in Treating Fe y NCT03873 Patients With PSCA+ Recrui Tim-3 Phase b CART mCRPC 23, 805 Metastatic Castration ting Biomarker 1 20 201 Resistant Prostate Cancer 21 9 Fecal Microbial Ma Fecal De Transplantation in r NCT03772 Recrui Th+ Tim-3 Melano Phase c Combination With 27, 899 ting Immuno Biomarker ma 1 20 Immunotherapy in 201 th 23 Melanoma Patients (MIMic) 9 Pembrolizumab TX-naive Jun Ju Distant Mets Melanoma NCT03089 Recrui Tim-3 Melano Phase e 1, ne and Use of AMT (PET) at PD-1 606 ting Biomarker ma 2 201 20 Baseline as Imaging 7 22 Biomarker Biomolecules 2020, 10, 750 5 of 9

Table S5. Clinical trials implicating galectins as biomarkers (5).

STA EN CLINICAL STATU TARGET BIOMARK TUMOR PHAS RESUL RT D TRIAL TITLE S S ERS TYPES ES TS DA DA NUMBERS TE TE Study to Assess Safety,Tolerability,Efficacy Dec Fe NCT04253 of PM01183 and Recrui PD-L1 + Tim-3 Phase 13, b NSCLC 145 in Patients w/ ting DNA Biomarker 1 201 20 Advanced Small Cell Lung 9 22 Cancer. Nivolumab in Treating July M NCT03121 Patients With Advanced Withd Tim-3 Phase 21, ar PD-1 NSCLC 417 Metastatic Non-small Cell rawn Biomarker 2 201 20 Lung Cancer 7 19 Phase July Ju NCT01567 CT Antigen TCR-redirected T Compl Immuno Tim-3 Ovarian 1| 9, ne 891 Cells for . eted th Biomarker Cancer Phase 201 20 2 3 17 Active, July Jul NCT03618 Trial of eRapa in Prostate not Tim-3 Phase 20, y Pca 355 Cancer Patients recruit Biomarker 1 201 20 ing 8 20 and Pembrolizumab Apr M Active, in Subjects With Advanced PD-1 il arc NCT02636 not Tim-3 Sarcoma Phase Alveolar Soft Part Sarcoma +Chemo 19, h 725 recruit Biomarker s 2 and Other Soft Tissue th 201 20 ing Sarcomas 6 21 Study of Anlotinib Hydrochloride and Not July Jul NCT03946 Toripalimab in Subjects yet Tim-3 Sarcoma Phase 19, y PD-1 943 With Unresectable or recruit Biomarker s 2 201 20 Metastatic Undifferentiated ing 9 23 Pleomorphic Sarcoma A Study of LY3321367 Alone Apr Active, Ju or With LY3300054 in il NCT03099 not Tim-3 Solid Phase ne Participants With Advanced PD-L1 12, 109 recruit Biomarker Tumor 1 20 Relapsed/Refractory Solid 201 ing 20 Tumors 7 Stoppe d Nov Oc A Study of LY3415244 in withou NCT03752 Termi Tim-3 Solid Phase 22, t Participants With Advanced PD-L1 t 177 nated Biomarker Tumor 1 201 20 Solid Tumors public 8 19 explan ation. Study of BGB-A425 in Phase Nov De NCT03744 Combination With Recrui Tim-3 Solid 1| 13, c - 468 Tislelizumab in Advanced ting Biomarker tumors Phase 201 20 Solid Tumors 2 8 21 Biomolecules 2020, 10, 750 6 of 9

Table S6. Clinical trials implicating galectins as biomarkers (6).

STA EN CLINICAL STATU TARGET BIOMARK TUMOR PHAS RESUL RT D TRIAL TITLE S S ERS TYPES ES TS DA DA NUMBERS TE TE

2 out of 6 A Phase 1/2 Study of PXD101 patient () in Combination HDAC s Phase Mar Oc With , +Radiot Thymic experie NCT01100 Termi Tim-3 1| 4, t and in h malignac nced a 944 nated Biomarker Phase 201 20 the First Line Treatment of +Chemo ies dose 2 0 15 Advanced or Recurrent th limitin Thymic, Malignancies g toxicity (DLT).

Study of , TSR-022, Active, PD-1 + Oct Fe , and Platinum- NCT03307 not VEGF Tim-3 Phase 12, b Based Doublet Various 785 recruit +Chemo Biomarker 1 201 20 in ing th 7 21 Combination With TSR-042

Phase Feb Oc A Phase 1/2 Safety Study of NCT03058 Recrui Chemot Tim-3 1| 9, t Intratumorally Dosed Various 289 ting h Biomarker Phase 201 20 INT230-6 2 7 22

A Study to Compare Oct Jan Treatments for a Type of NCT03595 Recrui Tim-3 Phase 9, 9, Kidney Cancer Called multiple Various 124 ting Biomarker 2 201 20 TFE/Translocation Renal Cell 8 24 Carcinoma (tRCC)

Intratumoral AST-008 Phase Dec Ap PD-1 NCT03684 Combined With Recrui Tim-3 1| 13, r + Anti- Various 785 Pembrolizumab in Patients ting Biomarker Phase 201 20 TLR9 With Advanced Solid Tumors 2 8 21 Biomolecules 2020, 10, 750 7 of 9

Table S7. Clinical trials using galectins inhibitors (1).

STA EN CLINICAL STATU TARGET BIOMARK TUMOR PHAS RESUL RT D TRIAL TITLE S S ERS TYPES ES TS DAT DA NUMBERS E TE A Phase 1, First-in-man Study Ma of OTX008 Given Unkno Feb NCT017243 Solid Phase y Subcutaneously as a Single wn Gal-1 201 20 Tumors 1 20 Agent to Patients With status 2 13 Advanced Solid Tumors A New Agent GM-CT-01 in Combination With 5-FU, Colorect Oct NCT003887 Withdr Galectin Gal-3 Phase Avastin and Leucovorin in al 200 00 awn s Biomarker 2 Subjects With Colorectal Cancer 6 Cancer GCS-100LE in Combination Phase Ap With and July NCT007768 Withdr Lympho 1 r Dexamethasone in Relapsed Gal-3 200 02 awn ma Phase 20 or Refractory Diffuse Large B- 8 2 09 Cell Lymphoma Metastat Phase Ap Apr NCT017238 Peptide Vaccinations Plus Termin Gal-3 ic 1 [1–2] r 201 13 GM-CT-01 in Melanoma ated +Vaccine Melano Phase 20 2 ma 2 15 Effect of Modified Citrus Jun Prostatic Jan NCT016818 Pectin on PSA Kinetics in Compl Phase [3–8] e Gal-3 Neoplas 20 23 Biochemical Relapsed PC eted 2 201 ms 20 With Serial Increases in PSA 3

Table S8. Clinical trials using galectins inhibitors (2).

STA EN CLINICAL STATU TARGET BIOMARK TUMOR PHAS RESUL RT D TRIAL TITLE S S ERS TYPES ES TS DA DA NUMBERS TE TE 2 out of 6 A Phase 1/2 Study of patient PXD101 (Belinostat) in s HDAC Combination With Cisplatin, Phase experi Ma Oc +Radiot Thymic NCT01100 Doxorubicin and Termi Tim-3 1 enced r 4, t h maligna 944 Cyclophosphamide in the nated Biomarker Phase a dose 201 20 +Chemo cies First Line Treatment of 2 limitin 0 15 th Advanced or Recurrent g Thymic, Malignancies toxicit y (DLT). Study of Niraparib, TSR-022, Active, PD-1 Oct Fe Bevacizumab, and Platinum- NCT03307 not + VEGF Tim-3 Phase 12, br Based Doublet Various 785 recruit +Chemo Biomarker 1 201 20 Chemotherapy in ing th 7 21 Combination With TSR-042 Phase Feb Oc A Phase 1/2 Safety Study of NCT03058 Recrui Chemot Tim-3 1 9, t Intratumorally Dosed Various 289 ting h Biomarker Phase 201 20 INT230-6 2 7 22 A Study to Compare Oct Ja Treatments for a Type of NCT03595 Recrui Tim-3 Phase 9, n Kidney Cancer Called multiple Various 124 ting Biomarker 2 201 20 TFE/Translocation Renal Cell 8 24 Carcinoma (tRCC) Intratumoral AST-008 Phase Dec Ap Combined With PD-1 NCT03684 Recrui Tim-3 1 13, r Pembrolizumab in Patients + Anti- Various 785 ting Biomarker Phase 201 20 With Advanced Solid TLR9 2 8 21 Tumors Biomolecules 2020, 10, 750 8 of 9

Table S9. Clinical trials using galectins inhibitors (3).

STA EN CLINICAL STATU TARGET BIOMARK TUMOR PHAS RESUL RT D TRIAL TITLE S S ERS TYPES ES TS DA DA NUMBERS TE TE A Phase 1 Study of TSR-022, Jun an Anti-TIM-3 Monoclonal July NCT02817 Recruit Solid Phase e Antibody, in Patients With TIM-3 201 633 ing Tumors 1 20 Advanced Solid Tumors 6 22 (AMBER) A Safety and Tolerability Aug Jan NCT03652 Study of INCAGN02390 in Recruit Phase 29, TIM-3 Various 20 077 Select Advanced ing 1 201 21 Malignancies 8 Stoppe GM-CT-01 Plus 5- d Ma Ma Colorect NCT00110 as Third- or Fourth-Line Termin Galectin Phase withou y r al 721 Therapy for Metastatic ated s + ADN 2 t public 200 20 Cancer Colorectal Cancer explan 5 12 ation. Safety of GM-CT-01 With and Feb NCT00054 Compl Galectin Phase Without 5-Fluorouracil in various 200 977 eted s + DNA 1 Patients With Solid Tumors 3 Stoppe Galectin Inhibitor (GR-MD- Metasta d and Ma No Galectin NCT02117 02) and Ipilimumab in Compl tic Phase Contin y 8, v s (Gal-3) 362 Patients With Metastatic eted Melano 1 ued by 201 20 + PD-1 Melanoma ma NCT02 4 18 575404 GR-MD-02 Plus Ma Pembrolizumab in Galectin y NCT02575 Melanoma, Non-small Cell Recruit Phase s (Gal-3) Various 16, 404 Lung Cancer, and Squamous ing 1 + PD-1 201 Cell Head and Neck Cancer 6 Patients Biomolecules 2020, 10, 750 9 of 9

Reference

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