Aceglatone (Glucaron/ 2.5-Di-O-acetyl-D-glucaro-1,4:6,3-dilactone/ DAGDL ) is a non-toxic natural inhibitor of beta-glucuronidase. Is an antineoplastic drug available in Japan, which is used for preventive therapy after preservative operation against bladder cancer.

Estriol acetate benzoate is a semisynthetic, steroidal estrogen. Estriol benzoate diacetate is reported as an ingredient of Holin in Japan. It is an estrogen receptor agonist.

Midecamycin diacetate (a derivative of Midecamycin) is reported as an ingredient of Miocamycin in Japan. Miocamycin is an orally administered 16-membered macrolide antimicrobial drug. It has a spectrum of in vitro activity similar to that of erythromycin, inhibiting a range of Gram-positive and Gram-negative organisms, atypical microbes and some anaerobes. Importantly, miocamycin demonstrates greater in vitro potency than erythromycin against several pathogens including Legionella pneumophila, Mycoplasma hominis, and Ureaplasma urealyticum. Equally noteworthy is its activity against erythromycin-resistant staphylococcal and streptococcal species expressing inducible-type resistance. Miocamycin possesses poor overall activity against Haemophilus influenzae and is inactive against Enterobacteriaceae. Penetration of miocamycin into body tissues and fluids is both rapid and extensive. The 3 major metabolites of miocamycin possess antimicrobial activity and may contribute to the therapeutic efficacy of the drug. Clinical data indicate that miocamycin is useful in the treatment of upper and lower respiratory tract infections in both adult and paediatric patients. Miocamycin is also effective in the treatment of urogenital tract infections caused by Chlamydia trachomatis or U. urealyticum. Midecamycin binds reversibly to 50S ribosomal subunit causing blockade of transpeptidation/translocation reactions, inhibition of protein synthesis and thus inhibition of cell growth. Midecamycin diacetate is also known as MIOCAMEN, Merced Box of 8 sachets (900mg), Mosil, Myoxam.

Hexestrol diacetate (brand name Retalon-Lingual among others) is an ester of hexestrol. It is a synthetic estrogen that was used for the treatment of menstruation disorder. It is an estrogen receptor agonist. A single therapeutic dose of hexestrol diacetate administered in impuber sheep has been shown to induce massive follicular atresia. So the incorrect utilisation of some hormonal formulations and the consumption of forages that contain estrogen like compounds, can represent major causes of infertility in sheep.

Cyclofenil is a anti-estrogen drug developed for the treatment of female infertility and for induction of ovulation. Cyclofenil exerts its action by binding to estrogen receptor beta and demonstrates agonism or antagonism depending on tissues type. The drug was withdrawn from the market due to high risk of hepatotoxicity.

Dipyrocetyl (2,3-diacetyloxybenzoic acid) is a drug used as an analgesics and antipyretics. Besides, was shown, that it may be useful in the treatment of acute lung injury (ALI) associated with acute respiratory distress syndrome (ARDS). Dipyrocetyl possesses the anticoagulation properties, which may contribute directly to improve tissue integrity as well as indirectly by the prevention of activation of pro-inflammatory cytokines. In addition, was made a suggestion, that the drug may function as an MMP inhibitor.

Acreozast is an orally active antiallergic agent, which has anti-inflammatory activity. It was undergoing phase II clinical trials in Japan for the following condition: Asthma and Atopic dermatitis. Toyobo discontinued the development of acreozast in 1996.

Lonapalene (6-chloro-2,3-dimethoxynaphthalene-1,4-diol-diacetate; RS-43179) is a topically effective 5-lipoxygenase inhibitor. Lonapalene was shown to inhibit platelet cyclooxygenase. Lonapalene has been studied in the treatment of psoriasis. Development of lonapalene has been discontinued.

Acetomenaphthane, A vitamin K analogue used to treat and prevent hypoprothrombinemia caused by vitamin K deficiency. Also called menadiol diacetate. Hypoprothrombinemia is a blood disorder in which a deficiency of prothrombin results in impaired blood clotting, leading to an increased physiological risk for bleeding, especially in the gastrointestinal system, cranial vault, and superficial integumentary system.