QAV-680 is a pyrrolopyridine derivative patented by Novartis Pharma GmbH as chemoattractant receptor (CRTh2) antagonist for the treatment of an inflammatory or allergic condition, particularly an inflammatory or obstructive airways disease. QAV-680 shows low nM potency and excellent selectivity across a range of CRTh2 dependent primary human inflammatory cell assays. In preclinical studies, QAV-680 shows good pharmacokinetic properties (including a suitable escalating dose–exposure relationship) in the rat and mouse and demonstrates efficacy in both mechanistic and allergic disease CRTh2-dependent rodent in vivo models. In 2008-2010 QAV-680 was tested in Phase 2 clinical trials but no further development reports were published.

HM-30181 is a highly selective and potent inhibitor of Multi-drug resistance 1 (MDR1, ABCB1), also known as P-glycoprotein (P-gp). Co-administration of HM30181 greatly increased oral bioavailability of tubulin-stabilizing chemotherapeutic agent paclitaxel. Oraxol is an oral dosage form of paclitaxel administered orally with the HM30181A molecule. Oraxol offers patients with paclitaxel-responsive tumors the possibility of oral therapy without the requirement for premedication to prevent infusion-related hypersensitivity-type reactions. Current clinical data suggests the promising potential of a better clinical response and tolerability profile, which can likely to be attributed to the better pharmacokinetic profile achieved. Oraxol is presently in a Phase 3 trial in metastatic breast cancer and poised to enter into a combination study for treatment of advanced gastric cancer with ramucirumab through a clinical trial collaboration with Eli Lilly and Company.

Acebilustat (formerly CTX-4430) is an investigational oral drug under development by Celtaxsys. It is a potent inhibitor of the enzyme leukotriene A4 hydrolase (LTA4H), which catalyzes the rate‐limiting step in the formation of leukotriene B4 (LTB4), a potent chemoattractant and activator of inflammatory immune cells including neutrophils. Acebilustat is currently being tested in Phase 2 clinical trial as a modulator of inflammation in patients with cystic fibrosis (CF). The U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have granted orphan drug status to acebilustat as a treatment for cystic fibrosis.