VTP-27999 is an alkyl amine renin inhibitor. This compound demonstrated excellent selectivity over related and unrelated off-targets, >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans. Vitae Pharmaceuticals was developing VTP 27999 for the treatment of chronic kidney disease. VTP 27999 was in phase I clinical development in the US. However, the product is no more on the company pipeline and it appears that the development has been discontinued.

Ampion (LMWF-5A) is a low molecular weight fraction of human serum albumin (HSA) currently being developed for the treatment of pain due to osteoarthritis of the knee. The primary constituent ingredient of Ampion is aspartyl-alanyl diketopiperazine, or DA-DKP, an endogenous immunomodulatory molecule derived from the N-terminus of HSA. Based on published pre-clinical and clinical research, DA-DKP plays a significant role in the regulation of inflammation. DA-DKP is believed to reduce inflammation by suppressing pro-inflammatory cytokine production in T-cells. Ampion also contains other known small molecules that confer anti-inflammatory effects to complement the activity of DA-DKP and derive demonstrated in-vitro and in-vivo effects. Ampio is currently developing Ampion as an intra-articular injection to treat osteoarthritis of the knee, and the final US pivotal trial is underway. Additional pre-clinical and clinical studies have been completed or are underway for Ampion and other chronic inflammatory conditions.

Domitroban is a phenylsulfony;aminobicycloheptenoic acid derivative. It is a thromboxane A2 receptor antagonist. It is a potential antiasthmatic and an experimental cerebroprotective drug. It inhibits proteinuria in animal models of renal injury. Calcium salt of R-domitroban had been in phase II clinical trial for the treatment of allergic rhinitis. Also, it was in preregistration stage for the treatment of asthma in Japan. However, these studies were discontinued.

Ajulemic acid, designated as Resunab™, is being developed by Corbus Pharmaceuticals, for the treatment of cystic fibrosis, systemic sclerosis, systemic lupus erythematosus.Ajulemic acid (AJA) is a first-in-class, synthetic, orally active, cannabinoid-derived drug that preferentially binds to the CB2 receptor and is nonpsychoactive. In preclinical studies, and in Phase 1 and 2 clinical trials, AJA showed a favorable safety, tolerability, and pharmacokinetic profile. It also demonstrated significant efficacy in preclinical models of inflammation and fibrosis. It suppresses tissue scarring and stimulates endogenous eicosanoids that resolve chronic inflammation and fibrosis without causing immunosuppression. AJA is currently being developed for use in 4 separate but related indications including systemic sclerosis (SSc), cystic fibrosis, dermatomyositis (DM), and systemic lupus erythematosus. Phase 2 clinical trials in the first 3 targets demonstrated that it is safe, is a potential treatment for these orphan diseases and appears to be a potent inflammation-resolving drug with a unique mechanism of action, distinct from the nonsteroidal anti-inflammatory drug (NSAID), and will be useful for treating a wide range of chronic inflammatory diseases.

Melarsonyl is an arsenical anthelmintic compound. It has been used for the treatment of human trypanosomiasis and onchocerciasis.

Radalbuvir (also known as GS-9669 ) is a Hepatitis C virus NS 5 protein inhibitor for the treatment of hepatitis C virus (HCV) infection developed by Gilead Sciences. Radalbuvir is a highly optimized thumb site II nonnucleoside inhibitor, with a binding affinity of 1.35 nM for the genotype (GT) 1b protein. It is a selective inhibitor of HCV RNA replication, with a mean 50% effective concentration of ≤ 11 nM in genotype 1 and 5 replicon assays, but lacks useful activity against genotypes 2 to 4. In preclinical Radalbuvir exhibited at least additive activity in combination with agents encompassing four other direct modes of action (NS3 protease, NS5A, NS5B via an alternative allosteric binding site, and NS5B nucleotide) as well as with alpha interferon or ribavirin in replicon assays. It exhibited high metabolic stability in vitro human liver microsomal assays, which, in combination with its pharmacokinetic profiles in rat, dog, and two monkey species, is predictive of good human pharmacokinetics. In clinical trials, Radalbuvir shows highly effective inhibition of wild-type HCV.