Rosiptor (AQX-1125) is a once daily, orally administered small molecule being developed by Aquinox Pharmaceuticals for the treatment of asthma, bladder pain syndrome/interstitial cystitis (IC/BPS) and chronic prostatitis/chronic pelvic pain syndrome. AQX-1125 is the only clinical-stage, orally administered, SHIP1 activator. AQX-1125 significantly reduces the late response to allergen challenge, with a trend to reduce airway inflammation. AQX-1125 was safe and well tolerated and merits further investigation in inflammatory disorders. AQX-1125 has been used in trials studying the treatment of COPD, atopic dermatitis, interstitial cystitis, and bladder pain syndrome. However, the development has been discontinued.

Neoandrographolide, one of the principal diterpene lactones, isolated from a medicinal herb Andrographis paniculata Nees. Andrographis paniculata (Burm. f.) Wall. ex Nees (Acanthaceae), also known as “kalmegh” in India, is a widely distributed plant in Asia. In many traditional formulations, the aerial parts have been used as anti-inflammatory and antipyretic drugs for the treatment of a variety of chronic and infectious diseases. Neoandrographolide possesses significant anti-inflammatory effects, which implies that it would be one of the major contributing components to participate in the anti-inflammatory effect of A. paniculata. and a potential candidate for further clinical trial.

GSK 1059615, a pyridinylquinoline derivative, is a novel PI3K kinase and mTOR dual inhibitor. GSK1059615 was in phase I clinical trial in patients with solid tumors or lymphoma, but this study was terminated prematurely due to lack of sufficient exposure following single- and repeat dosing. In addition, recently was shown, that GSK 1059615 in xenograft mice models possessed anti-head and neck squamous cell carcinoma (HNSCC) cell activity.

METHYLENETETRAHYDROFOLIC ACID, L-(+), an endogenous biomodulator that was developed under the brand name modufolin or arfolitixorin by the Isofol Medical. Arfolitixorin is developed to increase the efficacy of standard of care chemotherapy for advanced colorectal cancer. This drug is currently being studied in a global phase 3 clinical trial. Besides, the drug successfully completed phase II as rescue therapy for osteosarcoma. 21 May 2019 Isofol Medical has received clinical patent protection for the arfolitixorinin USA. It relates to a method of increasing blood concentration of deoxyuridine, a blood biomarker for inhibition of tumor growth in human cancer treatment.

Nifuradene (NF-246), a chemotherapeutic nitrofuran, was first synthesized and reported in 1956. Nifuradene, a 5-Nitorofuran derivative, is an antibacterial drug. Early in vitro testing found it an effective chemotherapeutic agent against most of the common urinary pathogens. Subsequent in vivo studies found that this compound is well absorbed after oral administration in both animals and humans. Nifuradene was used for the treatment of urinary tract infections. The over-all cure rate was found to be best at doses exceeding 600 mg a day.

Nifuratrone is a nitrofuran which was used for the control of Salmonella choleraesuis in swine. It was also used for the treatment of gonorrhea.

PF-04457845 is a fatty acid amide hydrolase 1 inhibitor developed by Pfizer for the treatment of inflammatory and noninflammatory pain disorders. The drug was tested in phase II in patients with osteoarthritis of the knee, but found to have the same effect as placebo. It was also assessed in phase II clinical trial for its effect on marijuana withdrawal and Tourette syndrome.

Curcumol is one of the major components of the essential oil of Rhizome Curcumae with the structure of sesquiterpenoid hemiketal. It exhibits characteristics such as antitumor, ant proliferation, anti-inflammatory, anti-hepatic fibrosis, antioxidant, and antimicrobial activities with low cytotoxicity. Curcumol suppresses the Breast Cancer Cells, Colorectal Cancer Cell Line, lung adenocarcinoma cell lines and others. However, its effect and mechanisms against tumor metastasis are still unclear. Recently was discovered a preliminary mechanism the suppression of breast cancer cell metastasis by curcumol. This mechanism suggested the inhibition of MMP-9 via JNK1/2 and Akt (Ser473)-dependent NF-κB signaling pathways.