contraceptive

Ethisterone (17α-Ethynyltestosterone) is a progestogen hormone.

Norethisterone enanthate (NSC-9564) is a long-acting parenteral progestogen with antigonadotropic effects.

Norgestimate is an acetylated progestinused in combination with ethinyl estradiol as an oral contraceptive.

Nomegestrol acetate is a widely used progestin-like drug,which is characterized as a full agonist at the progesterone receptor

CDD-1102 HCl is a novel BRDT-BD4 / BRD2-BD1302 selective inhibitor that shows non-hormonal contraceptive potential in ex vivo experiments.

4-Nonylphenol polyethoxylate (Nonoxinol-9) is a typical surfactant used as a vaginal spermicide. Spermicides are locally acting non-hormonal contraceptives. When present in the vagina during intercourse, they immobilize/inactivate/damage and/or kill sperms without eliciting systemic effects. 4-Nonylphenol polyethoxylate has been in use for more than 30 years as an over-the-counter (OTC) drug in creams, gels, foams and condom lubricants. It is the most commonly used spermicidal contraceptive in the UK and the USA. In several European countries, spermicides are no longer on the market.

Ethynodiol diacetate (Ethynodiol acetate) is a synthetic progestational hormone utilized alone or combined with estrogens as an oral contraceptive.

Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.

Chlormadinone acetate (Gestafortin) is an orally active synthetic progestational hormone used often in combinations as an oral contraceptive.

Dienogest (STS 557) is an orally-active, semisynthetic, fourth generation, nonethinylated progestogen with antiproliferative, antiandrogenic, anti-inflammatory and antiangiogenic activities that is used in hormone therapy and as a female contraceptive.

Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.

Norethynodrel (Lynestrol) is a synthetic progestational hormone with actions and uses similar to those of PROGESTERONE. It has been used in the treatment of functional uterine bleeding and endometriosis. As a contraceptive, it has usually been administered in combination with MESTRANOL.

Gestodene (WL 70) is a progestogen hormonal contraceptive.

Norgestimate metabolite Norelgestromin (17-Deacylnorgestimate) is one of the active metabolites of norgestimate.It is a steroidal progestin used in contraceptive patches, where it is combined with the estrogen ethinyl estradiol.

Nomegestrol (TX 066 free base) is an orally available, selective and potent full agonist of the progesterone receptor with potent anti-estrogenic, partial anti-androgenic and anti-gonadotropic activity.Nomegestrol is also a contraceptive progestin and is used in the study of endometriosis and meningiomas.

CDD-2807 is a serine/threonine kinase 33 (STK33) inhibitor with an IC50 of 9.2 nM. In mice, CDD-2807 demonstrates no significant toxicity and can cross the blood-testis barrier without accumulating in the brain. It offers reversible contraceptive effects, indicating potential for development as a male contraceptive.

VU6032735 is a potent and subtype-selective inhibitor of the sperm-specific potassium channel 3 (SLO3), with IC50 values of 165 nM for human SLO3 (hSLO3) and 730 nM for mouse SLO3 (mSLO3). It also inhibits sodium channels and L-type calcium channels. VU6032735 maintains high tissue exposure in the oviduct post-fertilization and is used in contraceptive research.

CDD-2210 is an STK33 inhibitor with a Kd value of 0.1 nM and an IC50 value of 38 nM. Its inhibitory effects on off-target kinases are relatively weak, with IC50 values for CLK1, CLK2, CLK4, and RET being 1209 nM, 917 nM, 544 nM, and 746 nM, respectively. CDD-2210 is applicable for contraceptive research.

CDD-2212 is an STK33 inhibitor with a Kd of 1.9 nM and an IC50 of 999 nM. It exhibits weak inhibitory activity against off-target kinases, with IC50 values of 3223 nM for CLK1, 1555 nM for CLK2, 5884 nM for CLK4, and 1093 nM for RET. CDD-2212 is applicable in contraceptive research.

Cyclodiol is an estrogen. It is utilized for female birth control and can be combined with various progestogens as an oral contraceptive.

EP055 is a non-hormonal male contraceptive agent. It targets the EPPIN protein on the surface of sperm, thereby inhibiting the binding of anti-EPPIN antibodies to EPPIN, with an IC50 value of 1121 μM. By reducing the internal pH and Ca2+ levels of sperm, EP055 induces sperm aggregation and inhibits sperm motility (IC50 value of 199.5 μM). EP055 is applicable in the development of male contraceptives.

Algestone acetophenide (Neolutin) is progesterone that used in estrus synchronization and has been evaluated as an injectable contraceptive in combination with estradiol enanthate. It is also used therapeutically as a topical anti-inflammatory and is applied topically in the therapy of ACNE.

Drospirenone mixture with Ethinylestradiol is a female oral combined contraceptive containing 30 mcg (0.030 mg) Ethinyl Estradiol and 3 mg drospirenone (Androstenes).

Fenestrel is a synthetic, nonsteroidal estrogen that was developed as a postcoital contraceptive in the 1960s. Fenestrel is a seco analogue of doisynolic acid and a member of the cyclohexenecarboxylic acid series of estrogens.