Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is active metabolites of tamoxifen. This metabolite exhibits a 100-fold higher binding affinity to the estrogen receptor (ER) and are more effective in suppressing cell proliferation than tamoxifen. In humans, the conversion from tamoxifen to endoxifen is predominant. Endoxifenis is an orally active, selective estrogen receptor modulator (SERM) that was developed for the treatment of estrogen receptor-positive breast cancer. In addition, this drug possesses antimanic properties, what can be used in the treatment of patients with bipolar I disorder (BPD I).

Salvinorin A has been reported to be the most potent naturally occurring hallucinogen, with an effective dose in humans in the 200- to the 1,000-μg range when smoked; it has been reported to induce an intense hallucinatory experience in humans, with a typical duration of action being several minutes to an hour or so. Salvinorin A is a highly selective agonist of the kappa-opioid receptor (KOR) with few off-target effects. It is a potent and selective dilator of the cerebral vasculature, exhibits rapid penetration through the blood-brain barrier, has potent anti-inflammatory properties, and has the ability to preserve neurovascular unit integrity. As such, salvinorin A is an ideal compound for the prevention and treatment of cerebral vasospasm following subarachnoid hemorrhage.

LY2452473 is a selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activity. Upon oral administration, LY2452473 acts as an agonist in select tissues and organs, including skeletal muscle, bone and the penis, thereby binding to and activating androgen receptor (AR) while acting as an antagonist in the prostate, thereby blocking AR activation and AR-mediated cellular proliferation. This may improve muscle mass and strength, bone formation, and erectile dysfunction while not stimulating growth of the prostate. Eli Lilly was developing LY 2452473/tadalafil combination for the treatment of erectile dysfunction. In addition, Eli Lilly is studying the use of a targeted LY 2452473 therapy, as a possible improvement in quality of life for prostate cancer patients who have undergone radical prostatectomy.

Batefenterol, previously known as GSK961081, a bifunctional muscarinic (M2 and M3 receptors) antagonist β2-agonist that is developed for chronic obstructive pulmonary disease (COPD). The drug has successfully completed phase II clinical trials with clinically significant improvements in lung function. No new or unexpected safety signals were observed in this COPD population. The conclusion from the trial was following that batefenterol 300 µg might represent the optimal dose for Phase III studies.

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.

Artefenomel, a novel trioxolane, is a lead candidate for inclusion in a new antimalarial combination, specifically formulated for children. Artefenomel has been demonstrated curative in as little as one dose.

Etarfolatide (EC20) is a conjugate of folic acid and peptidic metal-chelating moiety. Technetium Tc99m radiolabeled etarfolatide is a folate-targeted molecular imaging agent that is being developed to non-invasively identify tumors that express folate receptors and that may respond to folate-targeted therapy. It is being co-developed as the companion imaging agent to Vynfinit® (vintafolide) and EC1456 (folate-tubulysin).

Glyphosate-isopropylammonium has herbicidal activity. Glyphosate-resistant (GR) soybeans have been developed so that products containing Glyphosate-isopropylammonium can be used as herbicides without harming the plant. Glyphosate-isopropylammonium is used in products such as Accord, Glyphomax and Durango. Because they contain the herbicide glyphosate, these products have been associated with a risk of developing cancer.

Nevanimibe (also known as PD-132301 and ATR101) is an acetyl-CoA C-acyltransferase (ACAT1) inhibitor. Millendo Therapeutics is currently advancing the development of nevanimibe for the treatment of two orphan adrenal diseases: classic congenital adrenal hyperplasia (CAH) and endogenous Cushing's syndrome (CS). Both of these diseases are associated with an overactive adrenal cortex causing excess steroid production. Millendo believes that nevanimibe represents an adrenal-specific approach that will address these diseases through the reduction of adrenal steroid production. Millendo is currently conducting Phase 2 clinical trial to assess the safety and efficacy of nevanimibe in subjects with endogenous Cushing’s syndrome and for the treatment of adult CAH.