Tribendilol is a beta-adrenoceptor antagonist. Tribendilol has significant antihypertensive action but is associated with a high incidence of orthostatic side effects.

ETC-159 (ETC-1922159) is an inhibitor of membrane-bound O-acyltransferase porcupine. Porcupine palmitoleates Wnt and this modification is essential for binding to chaperone WLS and Frizzled receptors and is therefore required for the activity of all Wnts. ETC-159 exerts antineoplastic properties both in vitro and in vivo due to inhibition of Wnt pathway. ETC-159 development has progressed to phase I clinical trial.

CUDC-305, is a novel heat shock protein 90 (HSP90) inhibitor with strong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L), including many non-small cell lung cancer (NSCLC) cell lines which are resistant to standard-of-care (SOC) agents. In both laboratory and animal testing, CUDC-305 demonstrated high potency in vitro and/or in vivo across a wide range of cancers. Most notably, Curis scientists observed complete tumor regression following oral administration of CUDC-305 in a mouse xenograft model of acute myelogenous leukemia (AML). Tumor regression has also been observed after treatment of CUDC-305 in mouse xenograft models of breast, non-small cell lung, gastric cancer and glioblastoma brain cancers. In this preclinical testing, the compound also demonstrated an ability to effectively cross the blood brain barrier, and demonstrated an ability to extend survival in an intracranial glioblastoma model. Early stage toxicity studies suggest that CUDC-305 appears to have a better therapeutic window than several leading Hsp90 inhibitors in clinical development.

Abediterol, a fast and long-acting β2-adrenoceptor agonist (LABA), is being developed by AstraZeneca, for the treatment of asthma and chronic obstructive pulmonary disease. The investigational drug is a long-acting beta2-agonist (LABA) that has a bronchodilator effect, relaxing the muscles around the airways. It is currently under development and is in Phase II clinical trials.

Suncillin is an antibacteria and antifungal agent produced in Phytera's laboratory from a cell culture of a plant. Suncillin was patented by Bristol-Myers Co. In 1968 for the Pseudomonas bacteria treatment but was never marketed.

Solabegron (GW427353), a beta-3 adrenoceptor agonist, is in development with AltheRx (now Velicept Therapeutics) for the treatment of irritable bowel syndrome (IBS) and overactive bladder (OAB). Solabegron was discovered and first developed by GlaxoSmithKline. It was acquired by AltheRx, which merged with Velicept in 2015 to continue development of the program. Solabegron has been tested in over 800 study subjects in a twice-a-day formulation and demonstrated efficacy in the treatment of OAB as well as IBS. A once daily formulation designed to optimize patient convenience as well as efficacy has been developed and is currently being evaluated in a phase 2b dose ranging clinical trial. A Phase 2b dose ranging study with the twice daily formulation also began enrollment in Q1 2018.

Tiprenolol (DU21445) has been shown by both in vitro and in vivo animal experiments, to possess strong beta-adrenergic blocking but a relatively less strong negative inotropic activity. The same report also demonstrated by its inhibiting influence on spontaneous mobility of rat uterus, an intrinsic beta-sympathomimetic activity. Tiprenolol reveals effects similar to propranolol. Tiprenolol was shown to have significantly less heart rate slowing effect at rest than propranolol. However, all other measurements failed to show any difference of statistical significance between the two drugs with respect to any negative inotropic or beta‐blocking activity. The administration of tiprenolol or propranolol depressed the arterial pressure and caused the deaths of some dogs in which a coronary artery had been ligated.

Tigemonam is a dialkylazetidinone derivative patented by E. R. Squibb and Sons, Inc. as a beta-lactam agent useful for the treatment of bacterial infections. Of the orally active beta-lactams, tigemonam is one of the most potent, with a spectrum of activity similar to that of aztreonam and highly resistant to hydrolysis by the beta-lactamase enzymes. Tigemonam inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin.

Cefetecol is a broad-spectrum cephemcarboxylate derivative with antibacterial activity patented by British pharmaceutical company Glaxo Group Ltd.