Alvocidib (also known as Flavopiridol or HMR-1275) is a flavonoid alkaloid CDK9 kinase inhibitor under clinical development for the treatment of acute myeloid leukemia, by Tolero Pharmaceuticals, Inc. As a broad spectrum CDK inhibitor, Alvocidib can inhibit cell cycle progression in either G1 or G2 and induces G1 arrest in either MCF-7 or MDA-MB-468 cells by inhibition of the CDK4 or CDK2 kinase activity. Alvocidib exhibits potent cytotoxicity against a wide variety of tumor cell lines (LNCAP, HCT116, A2780, K562, PC3, and Mia PaCa-2) with IC50 values ranging from 16 nM for LNCAP to 130 nM for K562. Administration of Alvocidib at 7.5 mg/kg for 7 days displays slight antitumor activity against P388 murine leukemia, and active against the human A2780 ovarian carcinoma implanted sc in nude mice). Alvocidib treatment at 1-2.5 mg/kg for 10 days significantly suppresses collagen-induced arthritis in mice in a dose-dependent manner, by inhibiting synovial hyperplasia and joint destruction, whereas serum concentrations of anti-collagen type II (CII) Abs and proliferative responses to CII are maintained. Tolero Pharmaceuticals Inc. announced that the FDA has granted orphan drug designation for Alvocidib, its cyclin-dependent kinase small molecule inhibitor, for the treatment of patients with acute myeloid leukemia.

IVA-337 (LANIFIBRANOR), an indole sulfonamide derivative, is a pan peroxisome proliferator-activated receptor (PPAR) agonist. It is under investigation in Phase 2 clinical trials for non-alcoholic steatohepatitis, non-alcoholic fatty liver disease, and type 2 diabetes.

LANCOVUTIDE, also known as duramycin, is a 19-amino-acid tetracyclic peptide antibiotic. It is in clinical development for the treatment of cystic fibrosis (CF). It activates an alternative chloride channel in lung epithelial cells by elevating intracellular calcium levels, and may potentially compensate for CF transmembrane conductance regulator deficiency in the airway epithelium and increase the volume of the airway surface liquid.

Cibinetide (ARA 290; helix B surface peptide) is a novel potent and selective peptide agonist of innate repair receptor (IRR) with anti-inflammatory and tissue-protective activities. IRR activation promotes tissue protection and repair in a wide variety of preclinical models, including diabetic wound healing, diabetic neuropathy, and ischemic retinopathy. In a mouse model of diabetic small nerve fiber loss, daily administration of Cibinetide reversed neuronal dystrophy. Cibinetide administration significantly improved re-epithelization, angiogenesis, and wound healing strength in a mouse model of diabetic wounds. In clinical studies, Cibinetide administration has shown significantly increased small nerve fiber abundance, reduced neuropathic symptoms and promoted nerve fiber repair in patients with sarcoidosis or diabetes-related nerve fiber loss.