TABLE II.
Agonistic and antagonistic immune checkpoint modulators currently under investigation
| Target | Drug | Company | Clinical phase |
|---|---|---|---|
| Costimulatory or agonist antibodies | |||
|
| |||
| 4-1BB (CD137) | Utomilumab | Pfizer Canada, Kirkland, QC | I |
| Urelumab | Bristol–Myers Squibb, New York, NY, U.S.A. | I/II | |
| INBRX-105 | Inhibrx, San Diego, CA, U.S.A. | I | |
|
| |||
| ICOS (CD278) | GSK3359609 | GlaxoSmithKline, Mississauga, ON | I/II |
| JTX-2011 | Jounce Therapeutics, Cambridge, MA, U.S.A. | I/II | |
|
| |||
| GITR (CD357) | TRX 518-001 | Leap Therapeutics, Cambridge, MA, U.S.A. | I/II |
| MK-4166 | Merck, Kenilworth, NJ, U.S.A. | I | |
| BMS-986156 | Bristol–Myers Squibb, New York, NY, U.S.A. | I/II | |
| INCAGN01876 | Incyte Biosciences International, Wilmington, DE, U.S.A. | I/II | |
|
| |||
| CD70 | ARGX-110 (cusatuzumab) | Argenx, Breda, Netherlands | I/II |
|
| |||
| CD27 | CDX-1127 (varlilumab) | Celldex Therapeutics, Hampton, NJ, U.S.A. | I/II |
|
| |||
| OX40 (CD134) | PF-0451860 | Pfizer Canada, Kirkland, QC | I/II |
| MEDI0562/6469/6383 | AstraZeneca Canada, Mississauga, ON | I | |
| GSK3174998 | GlaxoSmithKline, Mississauga, ON | I | |
| BMS-986178 | Bristol–Myers Squibb, New York, NY, U.S.A. | I/II | |
|
| |||
| CD40 | CP870893 | Pfizer Canada, Kirkland, QC | I |
|
| |||
| APX005M | Bristol–Myers Squibb, New York, NY, U.S.A. | I/II | |
| Co-inhibitory or antagonist antibodies | |||
|
| |||
| VISTA (B7-H5) | CA-170 | Curis, Lexington, MA, U.S.A. | I |
|
| |||
| CCR4 (CD194) | Mogamulizumab | Kyowa Kirin, Tokyo, Japan | I/II |
|
| |||
| B7-H3 (CD276) | MGD009 | Novartis Pharmaceutical, Ottawa, ON | I |
|
| |||
| 8H9 | Y-mAbs Therapeutics, New York, NY, U.S.A. | I | |
| TIM-3 | TSR-022 | Tesaro, Waltham, MA, U.S.A. | I |
| MBG453 | Novartis Pharmaceutical, Ottawa, ON | I/II | |
| Sym023 | Symphogen A/S, Ballerup, Denmark | I | |
| MEDI9447 (oleclumab) | AstraZeneca Canada, Mississauga, ON | I | |
|
| |||
| LAG-3 (CD223) | BMS-986016 (relatlimab) | Bristol–Myers Squibb, New York, NY, U.S.A. | I/II |
| IMP321 (eftilagimod alpha) | Prima BioMed, Sydney, Australia | II | |
| LAG525 | Novartis Pharmaceutical, Ottawa, ON | I/II | |
|
| |||
| KIR (2DL1–3) | Lirilumab | Bristol–Myers Squibb, New York, NY, U.S.A. | I/II |
|
| |||
| IDO-1,2 | Indoximod | NewLink Genetics, Ames, IA, U.S.A. | II |
| Epacadostat | Incyte Biosciences International, Wilmington, DE, U.S.A. | II | |
|
| |||
| TIGIT | Tislelizumab | BeiGene, Beijing, P.R.C. | I/II/III |
| BMS-986207 | Bristol–Myers Squibb, New York, NY, U.S.A. | I/II | |
| MTIG7192A | Genentech, San Francisco, CA, U.S.A. | II/III | |
| AB154 | Arcus Biosciences, Hayward, CA, U.S.A. | I/II | |
|
| |||
| A2aR | Ciforadenant | Corvus Pharmaceuticals, Burlingame, CA, U.S.A. | I |
|
| |||
| Transforming growth factor β | M7824 | EMD Serono, Rockland, MA, U.S.A. | I/II |
| Galunisertib | Eli Lilly and Company, Indianapolis, IN, U.S.A. | II | |
|
| |||
| CD47 | TTI-621 | Trillium Therapeutics, Mississauga, ON | I |
|
| |||
| CD73 | MEDI9447 (oleclumab) | AstraZeneca Canada, Mississauga, ON | I |
| Other pathways | |||
|
| |||
| Toll-like receptors | Poly-ICIC | Ludwig Institute for Cancer Research, New York, NY, U.S.A. | I |
| MGN1703 (lefitolimod) | Mologen, Berlin, Germany | I | |
| SD-101 | Dynavax Technologies Corporation, Emeryville, CA, U.S.A. | I/II | |
| DSP-0509 | Boston Biomedical, Cambridge, MA, U.S.A. | I/II | |
| Rintatolimod | Hemispherx Biopharma, Philadelphia, PA, U.S.A. | II | |
| CMP-001 | Checkmate Pharmaceuticals, Cambridge, MA, U.S.A. | II | |
|
| |||
| Interleukin 2 receptor | NKTR-214 | Nektar Therapeutics, San Francisco, CA, U.S.A. | I/II/III |
| RO6874281 | Hoffmann–La Roche, Basel, Switzerland | I/II | |
| THOR-707 | Synthorx, La Jolla, CA, U.S.A. | I/II | |
|
| |||
| Arginase inhibitors | CB-1158 | Incyte Corporation, Wilmington, DE, U.S.A. | I/II |
|
| |||
| Oncolytic peptides | LTX-315 | Lytix Biopharma, Oslo, Norway | II |
|
| |||
| Interleukin 10 | AM0010 (pegilodecakin) | Eli Lilly and Company, Indianapolis, IN, U.S.A. | I/II |
Poly-ICLC = polyinosinic-polycytidylic acid–poly–L-lysine carboxymethylcellulose.
