Repositioning Candidate Details
| Candidate ID: | R1230 |
| Source ID: | DB09124 |
| Source Type: | approved; withdrawn |
| Compound Type: | small molecule |
| Compound Name: | Medrogestone |
| Synonyms: | Medrogestone |
| Molecular Formula: | C23H32O2 |
| SMILES: | [H][C@@]12CC[C@](C)(C(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])C=C(C)C2=CC(=O)CC[C@]12C |
| Structure: |
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| DrugBank Description: | Medrogestone (INN), also known as 6,17α-dimethyl-6-dehydroprogesterone, is a progestational agent derived from 17-methylprogesterone. It was conceived as an alternative for an orally effective contraceptive option. It was developed by Ayerst, approved in Canada in 1969 and its current status is cancelled post-marketing. It was never approved by the FDA. |
| CAS Number: | 977-79-7 |
| Molecular Weight: | 340.507 |
| DrugBank Indication: | Medrogestone is indicated as adjunct to treat endometial shedding in menopausal women, to treat secondary amenorrhea, to induce menses and to treat dysfunctional uterine bleeding in adult and adolescent women. |
| DrugBank Pharmacology: | Medrogestone was created as a more potent and orally active option of progesterone. In pre-clinical trials, medrogestone was proven to have four times more progestational activity than progesterone with a similar duration effect than the one found for 17-hydroxyprogesterone. Medrogestone was also able to maintain pregnancy and prevented ovulation in ovariectomized rats. Administration of medrogestone, alone or with premarin, prevented pregnancy, as well as it suppressed ovarian weight increase by nearly 100% of the tested individuals. Medrogestone does not produce any androgenic effect but it presented a marked anti-androgenic effect. It did not present an oestrogenic effect, nor changes in organ weight or histological appearance in adrenal glands or thymus and it does not present any anti-inflammatory effects. |
| DrugBank MoA: | Medrogestone is a progestogen, thus its action is done under the same profile. These type of molecules are steroid hormones that bind and activate the progesterone receptor. Its action may involve the suppression of gonadotropic hormones from the anterior portion of the pituitary gland and secondary suppression of testosterone. Medrogestone presents structural similarities to testosterone which allows it to compete for the androgen-receptor-protein receptor sites in prostatic cells. Administration of medrogestone diminishes the response to endogenous hormones in tumor cells due to a reduction in hormone steroid receptors; this effect will translate into cytotoxic or antiproliferative effects. |
| Targets: | Progesterone receptor ligand |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class |
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