Zardaverine is a Phosphodiesterase 3/4 inhibitor. Zardaverine exhibits potent and selective antitumor activity against hepatocellular carcinoma both in vitro and in vivo independently of phosphodiesterase inhibition. Zardaverine may be also useful for both, bronchorelaxation and reduction of inflammation in asthma therapy.

Tenatoprazole, also known as TU-199, is a proton pump inhibitor drug candidate that was undergoing clinical testing as a potential treatment for reflux oesophagitis and peptic ulcer. Tenatoprazole has an imidazopyridine ring in place of the benzimidazole moiety found in other proton pump inhibitors, and has a half-life about seven times longer than other PPIs.

Neridronic acid, also known neridronate, is a bisphosphonate. In Italy it is used to treat Osteogenesis imperfecta and Paget's disease of bone. Neridronic acid treatment has been reported to be effective also in other skeletal diseases such as osteoporosis, algodystrophy, hypercalcemia of malignancy and bone metastasis. Neridronic acid has been developed only for parenteral use, and it is the only one used as intramuscular injection.

(+)-Cloprostenol sodium is a water soluble, synthetic analog of prostaglandin F2α (PGF2α). It is an FP receptor agonist and a potent luteolytic agent in rats and hamsters.

Limaprost, also known as ONO 1206 and OP1206, is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency. Limaprost is orally active. Limaprost reduces motor disturbances by increasing the production of insulin-like growth factor I in rats subjected to spinal cord injury.

(+)-Cloprostenol is a PGF2α agonist and a synthetic analog of prostaglandin F2α (PGF2α). (+)-Cloprostenol reliably induces luteolysis in luteal phase mares without evoking clinical side effects or a stress response. Note: pure (+)-Cloprostenol isopropyl ester is an oily material. For the convenience of use, this product is supplied as ethanol solution at concentration of 200mg / mL.

Bimatoprost isopropyl ester is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost.

Atosiban, also known as ORF 22164, RWJ 22164, is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Although initial studies suggested it could be used as a nasal spray and hence would not require hospital admission, it is not used in that form. It was developed by Ferring Pharmaceuticals in Sweden and first reported in the literature in 1985. Originally marketed by Ferring Pharmaceuticals, it is licensed in proprietary and generic forms for the delay of imminent pre-term birth in pregnant adult women.

Splenopentin, also known as SP-5, is a synthetic immunomodulating peptide corresponding to the region 32-34 of a splenic product called splenin (SP) and the thymic hormone thymopoietin (TP), respectively. Splenopentin can reproduce the biological activities of TP and SP, respectively.

Somatostatin, also known as growth hormone–inhibiting hormone (GHIH), is a peptide hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones. Somatostatin inhibits insulin and glucagon secretion. Somatostatin has two active forms produced by alternative cleavage of a single preproprotein: one of 14 amino acids (shown in infobox to right), the other of 28 amino acids which is the short form with another 14 amino acids at one end.

Sermorelin, also known as GHRH (1-29), is a growth hormone-releasing hormone (GHRH) analogue used as a diagnostic agent. It is a 29-amino acid polypeptide representing the 1–29 fragment from endogenous human GHRH, and is thought to be the shortest fully functional fragment of GHRH.[1] It is used as a diagnostic agent to assess growth hormone (GH) secretion. It is also used as doping agent in sports due to its correlation with increased growth of muscular and skeletal tissue.[citation needed] Sermorelin use is also hypothesized to improve deep rapid eye movement sleep.

Ornipressin is a vasoconstrictor, haemostatic and renal agent. Ornipressin (Por 8) is also an efficient alternative to counteract hypotension during combined general/epidural anesthesia. Ornipressin plus dopamine can be a useful therapeutic option in patients with HRS type 1, especially as bridge to liver transplantation.

Lysipressin Acetate is an analog of Vasopressin, a powerful vasopressor used to modulate blood pressure. An endogenous antidiuretic hormone in most mammalian species. It is released into the blood from nerve terminals in the posterior pituitary and median eminence. It is a neurotransmitter in the central nervous system and also implicated in a variety of physiological processes such as regulating water balance by antidiuretic action.

Insulinotropin, also known as GLP-1 (7-37) and Tglp-1, is a potent stimulator of insulin secretion at concentrations as low as 5 X 10(-11) M (3- to 10-fold increases over basal). GLP-I(1-37) had no effect on insulin secretion even at concentrations as high as 5 X 10(-7) M. The earlier demonstration of specific liberation of GLP-I(7-37) in the intestine and pancreas, and the magnitude of the insulinotropic effect at such low concentrations, suggest that GLP-I(7-37) participates in the physiological regulation of insulin secretion.

Felypressin is a Vasopressin 1 agonist, and will thus have effects at all Arginine vasopressin receptor 1As. Felypressin has equipotent pressure responses when compared with epinephrine, showing a greater extent of action. Felypressin is safe for hypertensive subjects, in particular those receiving atenolol.

Tenidap, also known as CP-66248, is a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory drug candidate that was under development by Pfizer as a promising potential treatment for rheumatoid arthritis, but Pfizer halted development after marketing approval was rejected by the FDA in 1996 due to liver and kidney toxicity, which was attributed to metabolites of the drug with a thiophene moiety that caused oxidative damage.

Deutetrabenazine, also known as SD-809 and Tetrabenazine-d6, is an investigational, oral, small-molecule inhibitor of vesicular monoamine 2 transporter, or VMAT2, that is designed to regulate the levels of a specific neurotransmitter, dopamine, in the brain. Deutetrabenazine is a deuterated tetrabenazine. SD-809 is being developed for the treatment of chorea associated with Huntington’s disease, a neurodegenerative movement disorder that impacts cognition, behavior, and movements. Teva is investigating the broad potential of SD-809 for treating additional movements disorders such as tardive dyskinesia and tics associated with Tourette syndrome.

Deslorelin is a gonadotropin releasing hormone super-agonist (GnRH agonist) also known as an LHRH agonist. It stops the production of sex hormones (testosterone and oestrogen). It is currently approved for use in veterinary medicine and is used to induce ovulation in mares as part of the artificial insemination process. It is also used to stabilize high-risk pregnancies, mainly of livestock. Unlike other GnRH agonists, which are mainly used to inhibit luteinizing hormone and follicle-stimulating hormone by their ultimate downregulation of the pituitary gland.

Hydrocinchonine is an Alkaloid from Olea europaea. Hydrocinchonine is found in fruits.

Levobupivacaine is a local anaesthetic drug belonging to the amino amide group. It is the S-enantiomer of bupivacaine. Levobupivacaine hydrochloride is commonly marketed by Abbott under the trade name Chirocaine. Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 percent less potent (by molarity) than racemic bupivacaine and has a longer motor block onset time.

Cetilistat, also known as ATL-962, is a drug designed to treat obesity. It acts in the same way as the older drug orlistat (Xenical) by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested.

Carisbamate, also known as JNJ-10234094, RWJ 333369 and YKP-509, is an antiepileptic candidate. Carisbamate has powerful disease-modifying effects in the lithium-pilocarpine model of temporal lobe epilepsy. Carisbamate inhibits glutamate transmission in the granule cell of the dentate gyrus. Carisbamate acutely suppresses spasms in a rat model of symptomatic infantile spasms.

Amifampridine is used as a drug, predominantly in the treatment of a number of rare muscle diseases. The phosphate salt of amifampridine is a more stable formulation that does not require refrigeration. In the United States, amifampridine is under investigation for the treatment of Lambert-Eaton myasthenic syndrome (LEMS). Amifampridine is also used to treat many of the congenital myasthenic syndromes, particularly those with defects in choline acetyltransferase, downstream kinase 7, and those where any kind of defect causes "fast channel" behaviour of the acetylcholine receptor.

GABOB, also known as γ-Amino-β-hydroxybutyric acid, β-hydroxy-γ-aminobutyric acid, β-hydroxy-GABA, is an anticonvulsant which is used for the treatment of epilepsy in Europe, Japan, and Mexico. It is also an endogenous active metabolite and analogue of the neurotransmitter γ-aminobutyric acid (GABA), and for this reason, may function as a neurotransmitter itself.

Remogliflozin etabonate, also known as GSK 189075A or GSK 189075, is a SGLT2 inhibitor under development for the treatment of type 2 diabetes. Remogliflozin etabonate is a pro-drug of remogliflozin. Remogliflozin inhibits the sodium-glucose transport proteins (SGLT), which are responsible for glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. Remogliflozin is selective for SGLT2.

Nesbuvir, also known as HCV-796 and VB-19796, is a potent and selective NS5B polymerase inhibitor with potent anti-hepatitis C virus activity in vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus. Enzyme assays yielded median inhibitory concentration (IC(50)) values of 0.01 to 0.14 microM for genotype 1, with half maximal effective concentration (EC(50)s) of 5 nM and 9 nM against genotype 1a and 1b replicons. HCV796 demonstrated potent anti-HCV activity consistently through enzyme inhibition assays, subgenomic replicon, and chimeric mouse studies.

Cariprazine, also known as RGH-188 and MP-214, is an antipsychotic drug received FDA approval on September 17, 2015. Cariprazine acts as a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor. Action on the dopaminergic systems makes it also potentially useful as an add-on therapy in major depressive disorder. Cariprazine is approved for schizophrenia and bipolar disorder. It has also been investigated as a potential adjunct in treatment-resistant major depressive disorder.

Drinabant, also known as AVE1625, is a selective CB1 receptor antagonist under investigation varyingly as a treatment for obesity, schizophrenia, Alzheimer's disease, Parkinson's disease, and nicotine dependence. AVE1625 may be useful to treat the cognitive deficits in schizophrenia and as a co-treatment with currently available antipsychotics. In addition, an improved side-effect profile was seen, with potential to ameliorate the EPS and weight gain issues with currently available treatments.

Indeglitazar, also known as PPM-204 and PLX-204, is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma under development for for Type 2 diabetes mellitus (T2DM).

Arhalofenate, also known as JNJ-39659100 and MBX102, ) is a selective, partial PPAR-γ agonist that lowers glucose in the absence of some of the side effects, such as weight gain and edema, that are observed with the TZDs. Arhalofenate also displays pronounced triglyceride lowering in preclinical rodent models and in humans.