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US 2006/0094698 A1 De Nijs Et Al US 20060094698A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0094698 A1 De Nijs et al. (43) Pub. Date: May 4, 2006 (54) SELF-ADMINISTERED CONTRACEPTIVE (30) Foreign Application Priority Data NECTION OF OLY SOLUTION May 30, 2002 (EP)........................................ O2O77126.7 (76) Inventors: Henrik De Nijs, Oss (NL); Hendrikus Adrianus Antonius Van Der Voort, Publication Classification Oss (NL); Dirk D. Leysen, Organon (NL) (51) Int. Cl. A6II 3/56 (2006.01) A6M 3L/00 (2006.01) (52) U.S. Cl. ............................................ 514/170; 604/500 Correspondence Address: INTERVET INC. PATENT DEPARTMENT (57) ABSTRACT PO BOX 318 MILLSBORO, DE 19966-0318 (US) The subject 1nVent1On provides a pharmaceutical formula tion in the form of an oily solution for injection to a subject comprising a contraceptively and/or therapeutically effec tive amount of a long-acting progestogen and a contracep (21) Appl. No.: 10/515,714 tively and/or therapeutically effective amount of a long acting androgen dissolved in a pharmaceutically acceptable (22) PCT Filed: May 23, 2003 oily medium wherein the injection is administered by the subject itself with a needle-less device, a mini-needle device (86). PCT No.: PCT/EPO3/SO192 or a pre-filled Subcutaneous syringe. Patent Application Publication May 4, 2006 Sheet 1 of 16 US 2006/0094,698 A1 Figure 1 Etonogestrel heptanoate (Etonogestrel enanthate) Etonogestrel pentadecanoate Patent Application Publication May 4, 2006 Sheet 2 of 16 US 2006/0094698 A1 Figure 2a -0-Etonogestrel -- Etonogestrel heptanoate -A-Etonogestrel undecanoate --Etonogestrelnonanoate time (days) Patent Application Publication May 4, 2006 Sheet 3 of 16 US 2006/0094698 A1 -0- Etonogestrel -HEtonogestrel heptanoate -A- Etonogestrel undecanoate - - Etonogestrelnonanoate time (days) Patent Application Publication May 4, 2006 Sheet 4 of 16 US 2006/0094698 A1 Figure 2b PK in male rabbits after one i.m. injection of indicated etonogestrel-esters 40 3O 2 O 1 O time (days) Etonogestrel heptanoate Etonogestrel nonanoate C10: Etonogestrel decanoate C11: Etonogestrel undecanoate C12: Etonogestrel dodecanoate C13: Etonogestrel tridecanoate Patent Application Publication May 4, 2006 Sheet 5 of 16 US 2006/0094,698 A1 Figure 3 Testosterone heptanoate (Testosterone enanthate) Testosterone undecanoate Patent Application Publication May 4, 2006 Sheet 6 of 16 US 2006/0094698 A1 Figure 4 120 100 80 60 -e-Te (20 mg/kg) -a-Tu (20 mg/kg) --MENT-u (20 mg/kg) | --MENT.B. (20 mg/kg) 30 40 days after injection Patent Application Publication May 4, 2006 Sheet 7 of 16 US 2006/0094,698 A1 Figure 5 s 250 mg Testosterone enanthale im, Not mel ange wwn www." (w (0.0 mg festostefore underanoate i.m. {i}) mg einsters: he bic:claig irr, O 2 4 a 14 16 fire weeks) Patent Application Publication May 4, 2006 Sheet 8 of 16 US 2006/0094698 A1 Figure 6 Completeness of injection 100 D IM-Needle 90 O IM-MJ SC-Needle 80 SC-MJ 70 60 50 40 30 20 1O O Good Wet Patent Application Publication May 4, 2006 Sheet 9 of 16 US 2006/0094698 A1 Figure 7 EXTREMELY INTENSE 7 VERY INTENSE SLIGHTLY INTENSE BARELY STRONG MODERATE MLD VERY MILD WEAK VERY WEAK FAINT NO PAIN SENSATION Patent Application Publication May 4, 2006 Sheet 10 of 16 US 2006/0094698 A1 Figure 8 Immediate Pain Scores IM-Needle IM-MJ SC-Needle SC-MJ PC0.05 Pain Patent Application Publication May 4, 2006 Sheet 11 of 16 US 2006/0094698 A1 Figure 9 Unpleasent Pleasent U ofP P P | | | | | | | | Very Mildly Neutral Mildly Very Extremely Moderately Slightly : Slightly Moderately Extremely Patent Application Publication May 4, 2006 Sheet 12 of 16 US 2006/0094698A1 Figure 10 injection Sensation 2.5 M-Needle IM-MJ 2 SC-Needle SC-MJ 1.5 P&O.05 1 0.5 O Sensation Patent Application Publication May 4, 2006 Sheet 13 of 16 US 2006/0094698 A1 Figure 11 Local Site Reactions (2hr) % Reporting No Reaction 1 OO O IM-Needle IM-MJ 90 SC-Needle SC-MJ 80 70 P&O.05 60 50 40 30 20 10 Pain Itching Redness Swelling Bruising Patent Application Publication May 4, 2006 Sheet 14 of 16 US 2006/0094698 A1 Figure 12 Local Site Reactions (24hr) % Reporting No Reaction 100 D IM-Needle IM-MJ 90 SC-Needle SC-MJ 80 70 P-0.05 60 50 40 30 20 10 Pain itching Redness Swelling Bruising Patent Application Publication May 4, 2006 Sheet 15 of 16 US 2006/0094698 A1 Figure 13 Local Site Reactions (5-7 days) % Reporting No Reaction 100 D IM-Needle IM-MJ 90 SC-Needle SC-MJ 80 70 P&O.05 60 50 40 30 20 10 Swelling Bruising Patent Application Publication May 4, 2006 Sheet 16 of 16 US 2006/0094698 A1 Figure 14 Subject Preferences 90 M-Needle IM-MJ 80 SC-Needle SC-MJ 70 P&O.05 60 50 40 30 20 10 & Guestion 1 Guestion 2 Guestion 3 Question 4 US 2006/0094698 A1 May 4, 2006 SELF-ADMINISTERED CONTRACEPTIVE 0011. However, the use of specific esters of etonogestrel INUECTION OF OLY SOLUTION for female contraception, female HRT and treatment/pre vention of gynaecological disorders has not been suggested. FIELD OF THE INVENTION 0012. There are also no disclosures of a male or female 0001. The subject invention concerns the field of (male contraceptive/HRT solution for self-injection which would and female) contraception and (male and female) hormone result in high compliance levels. Compliance is probably the replacement therapy (HRT). most important factor in contraceptive use; without good compliance even the best contraceptives are without effect. BACKGROUND 0013 There is therefore a need for a male and female 0002 Contraceptive methods for men and women are contraceptive which will have a high compliance rate in important for worldwide reproductive health. male and female Subjects undergoing contraception. 0003. However, no effective and efficient methods of 0014 High compliance depends on infrequent, painless male contraception are as of yet available. administration without side effects and without local site 0004 Male contraception seeks to suppress spermatoge reactions. nesis through the Suppression of the gonadotropins lutein izing hormone (LH) and follicle-stimulating hormone SUMMARY OF THE INVENTION (FSH). This results in a depletion of intratesticular testoster 0015 The subject invention provides a pharmaceutical one and cessation of spermatogenesis. formulation in the form of an oily solution for injection to a 0005 Administration of progestagen results in a dose Subject comprising a contraceptively and/or therapeutically dependent Suppression of pituitary gonadotrophins and con effective amount of a long-acting progestogen and a con sequently, a decrease in testosterone levels and a reversible traceptively and/or therapeutically effective amount of a inhibition of spermatogenesis. An exogenous androgen is long-acting androgen dissolved in a pharmaceutically required to compensate for the reduced testosterone levels. acceptable oily medium wherein the injection is adminis In the same way, male HRT can be accomplished, resulting tered by the subject itself with a needle-less device, a in replacement of testosterone by an exogenous androgen mini-needle device or a pre-filled Subcutaneous syringe and which is safer on the prostate than endogenous testosterone. wherein the injectable volume of the solution is less than 1 milliliter. 0006 The use of progestogens together with androgens for use as male contraceptives is known (Guerin and Rollet 0016. The subject invention further contemplates a use of (1988), International Journal of Andrology 11, 187-199). a long-acting progestogen and a long-acting androgen dis Solved in a pharmaceutically acceptable oily medium for the 0007. However, the use of specific esters of etonogestrel manufacture of an injectable pharmaceutical formulation for for male contraception and HRT has not been suggested. male contraception wherein the injection is administered 0008. In addition, the use of progestogens together with with a needle-less device, a mini-needle device or a pre estrogens for use in female contraception is known (M. filled subcutaneous syringe and wherein the injectable vol Tausk, J. H. H. Thijssen, T. B. van Wimersma Greidanus, ume of the solution is less than 1 milliliter. "Pharmakologie der Hormone', Georg Thieme Verlag, Stut 0017. The subject invention also provides a male contra tgart, 1986). ceptive kit for injection comprising a long-acting progesto 0009 Progestagens are widely used for female contra gen and a long-acting androgen dissolved in an oily medium ception and in female HRT. In contraception, the combina wherein the injection is administered by the subject itself tion progestagen-estrogen oral contraceptives are the most with a needle-less device, a mini-needle device or a pre widely used. Administration of such a combination results in filled subcutaneous syringe and wherein the injectable vol a number of effects: it blocks ovulation, it interferes with ume of the solution is less than 1 milliliter. phasic development of the endometrium which decreases the chance for Successful implantation, and it causes the cervical 0018. The subject invention further contemplates a mucus to become so viscous that it hinders sperm penetra method of male contraception comprising injecting a solu tion. Most progestagen-only-pills (POPs) aim at the last tion comprising a contraceptively and/or therapeutically mentioned effect only. effective amount of a long-acting progestogen and a con traceptively and/or therapeutically effective amount of a 0010 Female HRT is aimed at suppletion of endogenous long-acting androgen dissolved in an oily medium to a estrogen for the treatment of peri- and postmenopausal subject wherein the injection is administered by the subject complaints (hot flushes, vaginal dryness), and for prevention itself with a needle-less device, a mini-needle device or a of symptoms of long-term estrogen deficiency.
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