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. Author manuscript; available in PMC: 2022 Nov 14.
Published in final edited form as: Annu Rev Cancer Biol. 2021 Dec 22;6(1):123–146. doi: 10.1146/annurev-cancerbio-070620-103554

Table 1.

Therapeutic strategies in clinical oncology development for TGFβ signaling blockade

Approach Target(s) Drug Cancer type(s) Clinical phase Clinical trial number or reference
Antibody Blocking pan-TGFβ (TGFβ1, TGFβ2, and/or TGFβ3) Fresolimumab (pan-TGFβ) Relapsed pleural malignant mesothelioma II NCT01112293
With radiotherapy in metastatic breast cancer II NCT01401062
Renal cell carcinoma, melanoma, and glioma II NCT00356460, NCT00923169, NCT01472731
With targeted ablation radiotherapy for NSCLC II NCT02581787
SAR439459 With cemiplimab (anti-PD-1) for advanced-stage or unresectable solid tumors I/Ib NCT03192345, NCT04729725
NIS793 In combination with anti-PD-1 for advanced malignancies I/Ib NCT02947165
With bevacizumab, FOLFOX6, or FOLFIRI for second-line therapy of metastatic colon cancer II NCT04952753
In combination with SOC chemotherapy for first-line treatment of metastatic ductal pancreatic cancer III NCT04935359
In combination with SOC chemotherapy with/without spartalizumab (anti-PD-1) for first-line treatment of metastatic ductal pancreatic cancer III NCT04390763
GARP: TGFβ1 ABBV-151 With/without budigalimab (anti-PD-1) for locally advanced or metastatic solid tumors II NCT03821935
LAP: TGFβ1 SRK-181 Locally advanced or metastatic solid tumors I/Ib NCT04291079
Integrin αvβ8 PF06940434 Advanced or metastatic solid tumor malignancies with/without anti-PD-1 I/Ib NCT04152018
Ligand trap TGFβ1 and -3 AVID200 Advanced and metastatic cancers, recurrent/refractory NSCLC, HCC, rectal cancer, ovarian carcinosarcoma, and newly diagnosed malignant glioma I and II NCT03834662
Small-molecule inhibitor TGFβR1 Galunisertib Advanced and metastatic cancers, multiple myeloma, urothelial carcinoma, and myeloproliferative neoplasm I and II NCT02906397, NCT02452008, NCT02688712, NCT02423343, NCT02734160, NCT01220271, NCT01246986, NCT02672475, NCT03206177, NCT01373164, NCT01373164
Vactosertib Colorectal cancer and solid tumor I and II NCT04064190, NCT03143985, NCT03724851, NCT04103645, NCT03802084, NCT03732274, NCT03698825, NCT04258072, NCT02160106
LY3200882 Solid tumors I NCT04031872, NCT02937272, NCT02937272
PF-06952229 Advanced NSCLC, advanced/metastatic/recurrent cancers, glioblastoma, brain metastasis from lung cancer, and glioma I, II, and III NCT03685591
Bispecific molecule TGFβ1 and -3 plus PD-L1 Bintrafusp alfa Various; particularly for HPV+ cancers I, II, and III Multiple ongoing trials, although two trials terminated due to lack of phase III efficacy compared to competitors

Abbreviations: FOLFIRI, folinic acid, fluorouracil, and irinotecan; FOLFOX6, folinic acid, fluorouracil, and oxaliplatin; GARP, glycoprotein A repetitions predominant; HCC, hepatocellular carcinoma; HPV, human papilloma virus; LAP, latency-associated peptide; NSCLC, non-small-cell lung cancer; SOC, standard of care.