Apricitabine (ATC) is an investigational drug that was being studied for the treatment of HIV infection. Apricitabine belongs to a class (group) of HIV drugs called nucleoside reverse transcriptase inhibitors (NRTIs). NRTIs block an HIV reverse transcriptase. By blocking reverse transcriptase, NRTIs prevent HIV from multiplying and can reduce the amount of HIV in the body. In vitro studies have shown that apricitabine appears to work on certain HIV strains against which other FDA-approved NRTIs, such as lamivudine (brand name: Epivir), may no longer work. Apricitabine shows antiviral activity in vitro against HIV-1 strains and clinical isolates with mutations in the reverse transcriptase that confer resistance to other NRTIs, including M184V, thymidine analogue mutations (TAMs), nucleoside-associated mutations such as L74V and certain mutations at codon 69. Apricitabine has shown activity in treatment-experienced HIV-1-infected patients with NRTI resistance (with M184V and up to five TAMs) as well as in treatment-naive patients. The study of apricitabine as an HIV medicine was discontinued in 2016. The company developing the drug decided to stop their clinical trials due to a lack of funding and a lack of interest in apricitabine’s early access program.

Octasine is an antihistamine agent that has never been marketed.

Flavodic acid is a synthetic hydrosoluble derivative of natural flavonoids. It has been shown to reduce capiliary fragility and permeability. Sodium flavodate was marketed by the Italian pharmaceutical company Farmaceutici under tradename Pericel.

Liroldine was found effective against both extraintestinal and intestinal amoebiasis in animal models. Its activity against hepatic infection in golden hamsters is comparable with that of different derivatives of nitroimidazoles used for human treatment. Against intestinal amoebiasis in Wistar rats, the activity was superior to nitroimidazoles and chloroquine. Paramomycin was comparable and diloxanide furoate was marginally superior. The comparative in vitro and in vivo studies with standard marketed drugs and liroldine indicate an excellent profile of the compound against experimental amoebiasis.

Subathizone (also known as Berculon B) is a thiosemicarbazone derivative useful for the chemotherapy of tuberculosis. In preclinical models, Subathizone shows potent activity in experimental tuberculosis in the mouse. In clinical trial, Subathizone shows moderate efficacy and frequent adverse events. Gastrointestinal disturbances and progressive anemia were the most toxic effects, but liver dysfunction, malaise, depression and lassitude, exanthemata, and conjunctival irritation also occurred.

Sudexanox is a xanthone derivative patented by French pharmaceutical company Roussel-UCLAF for the treatment of allergy, allergic asthma, and asthmatic bronchitis. In preclinical studies, Sudexanox possesses potent activity in the IgE-induced rat passive cutaneous anaphylaxis model.

Tonazocine is a nonpeptide, partial delta-opioid agonist with mu antagonist properties and weak k agonist activity. Tonazocine augmented the efficacy of L-DOPA in the reserpine model. Tonazocine evoked a dose-related, ipsilateral rotation, consistent with augmentation of dopaminergic function on the unlesioned side. Tonazocine has a narcotic antagonist activity which is 90 times that of pentazocine and 5 times less than that of naloxone as measured by the antagonism of morphine analgesia in the rat tail-flick test. Total pain relief scores for tonazocine 4 mg were nearly identical with that of morphine sulfate 10 mg while 8 mg of tonazocine were superior to 10 mg of morphine. Drowsiness was the main adverse reaction of tonazocine. Tonazocine has undergone phase II clinical trials for postoperative pain and appeared to possess reasonable efficacy.

Diarbarone is the anticoagulant.

In the early stages of testing was shown that it is about 4 times more potent than gallopamil and 12 times more potent than verapamil in its effects on smooth muscle tone and labeled calcium uptake.