{"id":43560,"date":"2022-08-03T07:44:58","date_gmt":"2022-08-03T07:44:58","guid":{"rendered":"https:\/\/i-base.info\/htb\/?p=43560"},"modified":"2024-01-24T16:45:52","modified_gmt":"2024-01-24T16:45:52","slug":"early-data-on-injecting-cab-rpv-la-into-thigh-muscle","status":"publish","type":"post","link":"https:\/\/i-base.info\/htb\/43560","title":{"rendered":"Early data on injecting CAB\/RPV-LA into thigh muscle"},"content":{"rendered":"
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Kirk Taylor, HIV i-Base<\/strong><\/p>\n<\/div>\n

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\"\"<\/strong>AIDS 2022 included results from a phase 1 study looking at whether lateral thigh muscle could be an alternative injection site for long-acting cabotegravir\/rilpivirine-LA (CAB\/RPV-LA). [1]<\/span><\/b><\/p>\n<\/div>\n

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Current formulations involve injections into gluteal muscle every two months by a health worker. <\/span><\/b><\/p>\n<\/div>\n

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The study enrolled 15 HIV negative participants (9 men, 6 women). Median age was 33 years (range: 21 to 49) and 7\/15 were Black and 5\/15 Hispanic\/Latinx. Median weight was 93 kg (range 67 to 107) and BMI was 31 kg\/m2<\/sup> (range: 24 to 34).<\/span><\/p>\n<\/div>\n

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The study protocol involved daily oral lead-in (CAB 30 mg plus RPV 25 mg) for 28 days, followed by a 14-day washout and single 3 mL IM injections of CAB (600 mg) and RPV (900 mg) in the lateral thigh muscle. Pharmacokinetic (PK) parameters were observed for one year.<\/span><\/p>\n<\/div>\n

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Median and geometric mean were > 4 x protein adjusted IC90 for both drugs at week 8. Although some individuals dropped below this target, all remained above the IC90 at this timepoint.<\/span><\/p>\n<\/div>\n

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Median levels of both drugs dropped below the IC90 after approximately 18 weeks and became undetectable at 24 weeks for cabotegravir but remained detectable at 52 weeks for rilpivirine.<\/span><\/p>\n<\/div>\n

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At week 8, CAB and RPV levels were 5.3-fold and 2.4-fold higher than their PA-IC90 threshold. <\/span><\/p>\n<\/div>\n

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Low grade adverse events were reported by all 15\/15 participants and included injection site reactions (ISRs), chills and headache. Grade 3 ISRs were due to pain at the injection site. Pain was reported up to 4 days post-injection and this was participants generally reported as acceptable. <\/span><\/p>\n<\/div>\n

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These data indicate that giving LA formulations in thigh muscle achieves target plasma levels out to 8 weeks and that the injections were tolerable. \u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0<\/span><\/p>\n<\/div>\n

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comment\u00a0 <\/span><\/h3>\n<\/div>\n
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These early data are encouraging but need to be confirmed in larger numbers and in people living with HIV as HIV can affect PK.<\/b><\/p>\n<\/div>\n

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If alternative injection sites are validated, this might allow self-administration of therapies.<\/b><\/p>\n<\/div>\n

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Further studies are required to evaluate the potential of the thigh and other relevant muscles as potential injection sites.<\/b><\/p>\n

Full results from this study has subce been published. [2]<\/p>\n<\/div>\n

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References<\/p>\n<\/div>\n

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  1. Hang K et al. Pharmacokinetics and tolerability of cabotegravir and rilpivirine long-acting intramuscular injections to the vastus lateralis (lateral thigh) muscles of healthy adult participants. AIDS 2022 (Montreal). 29th July to 2nd August. E-poster EPB176.
    \n<\/span>https:\/\/programme.aids2022.org\/Abstract\/Abstract\/?abstractid=9906<\/a> (abstract)
    \n    https:\/\/conference.aids2022.org\/media-1455-pharmacokinetics-pk-and-tolerability-of-cabotegravir-cab-and-rilpivirine-rpv-long-acting-l<\/a> (e-poster)<\/li>\n
  2. Han K et al. harmacokinetics and tolerability of cabotegravir and rilpivirine long-acting intramuscular injections to the vastus lateralis<\/i> (lateral thigh) muscles of healthy adult participants.. Pharmacologu, December 2023.
    \n    https:\/\/orcid.org\/0000-0001-8010-9898<\/a> <\/span><\/span><\/span>\n
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    \n<\/p><\/div>\n<\/div>\n<\/div>\n<\/div>\n<\/div>\n<\/li>\n<\/ol>\n<\/div>\n","protected":false},"excerpt":{"rendered":"

    Kirk Taylor, HIV i-Base AIDS 2022 included results from a phase 1 study looking at whether lateral thigh muscle could be an alternative injection site for long-acting cabotegravir\/rilpivirine-LA (CAB\/RPV-LA). [1] Current formulations involve injections into gluteal muscle every two months …<\/p>\n","protected":false},"author":3,"featured_media":0,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[4,3,34],"tags":[320],"class_list":["post-43560","post","type-post","status-publish","format-standard","hentry","category-conference-reports","category-antiretrovirals","category-pk-and-drug-interactions","tag-world-aids-24-montreal-2022"],"_links":{"self":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts\/43560","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/users\/3"}],"replies":[{"embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/comments?post=43560"}],"version-history":[{"count":4,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts\/43560\/revisions"}],"predecessor-version":[{"id":47109,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts\/43560\/revisions\/47109"}],"wp:attachment":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/media?parent=43560"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/categories?post=43560"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/tags?post=43560"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}