As of February 2024, BOLD-100 was being tested in a Phase 1b/2a clinical trial in 117 patients with advanced gastrointestinal cancers in combination with the chemotherapy regimen FOLFOX.

[4] BOLD-100 was developed from the closely related ruthenium molecule KP1339 (also known as IT-139 or NKP-1339) which is also sodium trans-[tetrachlorobis (1H-indazole) ruthenate(III)], but has different manufacturing methods and purity profiles.

BOLD-100 inhibits GRP78 and alters the unfolded protein response (UPR), while also inducing reactive oxygen species (ROS), leading to DNA damage.

[8] The precursor molecule to BOLD-100, KP1339 was tested in a Phase 1 monotherapy clinical trial in heavily pretreated patients with advanced cancers.

Interim data presented at ASCO GI in January 2024 showed that BOLD-100 + FOLFOX was active and well-tolerated treatment in a heavily pre-treated Stage IV mCRC study population with 36 patients.