HaiHe Biopharma (Shanghai HaiHe Pharmaceutical) is developing simmitecan, an ester pro-drug of chimmitecan for the treatment of cancer. Simmitecan is in phase I development for solid tumours and colorectal cancer in China. Simmitecan (L-P) is a water-soluble ester prodrug of chimmitecan (L-2-Z) with potent anti-tumor activities in different experimental animals. Chimmitecan，a novel CPT derivative, exhibited potent antitumor activities both in vitro and in vivo by inhibiting topoisomerase I.

Uprosertib is an oral potent Akt inhibitor which acts equally on Akt1, Akt2 and Akt3. The drug is under clinical development in combination with trametinib for the treatment of different cancers, including melanoma, myeloma, breast, endometrial, cervical cancer, etc.

PAC-14028 was developed as a transient receptor potential vanilloid type 1 (TRPV1) antagonist. It is known that TRPV1 might be deeply associated with skin permeability barrier function, suggesting that modulation of TRPV1 might be beneficial for the skin disorders with barrier damages. Amorepacific developed a topical cream formulation of PAC-14028. This drug completed phase III clinical trial for the treatment of atopic dermatitis. In addition, PAC-14028 participated in phase II clinical trials to evaluate its safety and efficacy in seborrheic dermatitis and in rosacea. Moreover, PAC-14028 has been used in trials studying the treatment of pruritus.

Mallinckrodt (previously Sucampo Pharmaceuticals) is developing nobiprostolan (RK 023), a topical therapy for male pattern baldness (androgenetic alopecia) and hypotrichosis. The drug is a physiologically active fatty acid derivative. Nobiprostolan is in Phase IIa clinical trials for the treatment of male pattern baldness.

3-Pyridinecarboxylic acid, 1-(4-methylphenyl)ethyl ester is an choleretic agent.

Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5. Veledimex controls the expression of the target gene. The amount of gene product produced by the system and the duration of the effect is dependent on veledimex dose level and duration of dosing. Nonclinical studies demonstrated that intratumoral administration of Ad-RTS-IL12 along with oral administration of veledimex elicited dose-dependent anti-tumor effects in murine melanoma, breast cancer and glioma models which correlated with increased plasma exposure of veledimex. The FDA granted Fast Track designation for Ad-RTS-hIL-12 plus veledimex for the treatment of recurrent or progressive glioblastoma multiforme in adults. Ad-RTS-hIL-12 is an inducible adenoviral vector encoding human pro-inflammatory cytokine interleukin-12 (IL-12), which is under the transcriptional control of the RheoSwitch Therapeutic System. Veledixmex is an oral activator ligand. Data previously presented suggest that Ad-RTS-hIL-12 with 20 mg veledimex improves the median overall survival from 6 to 9 months seen with available therapies to 12.7 months, with further improvement in median overall survival to 17.8 months in a subset of subjects with reduced cumulative steroid exposure during the active dosing period of veledimex. Veledimex has been used in trials studying the treatment of glioblastoma multiforme, metastatic breast cancer, and anaplastic oligoastrocytoma.

Arverapamil (brand name Rezular), a modulator of melatonin and serotonin receptors, was developed by Ireland-based company, AGI Therapeutics. The drug participated in phase III of clinical trials for patients to treat the irritable bowel syndrome with diarrhea, the trial was discontinued because the drug didn’t meet the primary endpoint.