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Cabotegravir  Audio icon

Other Names: 744 LA, CAB, GSK-1265744, GSK1265744, GSK744, GSK744 LA, GSK744 LAP, S-265744, S/GSK1265744, cabotegravir LA, cabotegravir sodium
Drug Class: Integrase Inhibitors
Molecular Formula: C19 H17 F2 N3 O5
Registry Number: 1051375-10-0 (CAS)
Chemical Name: (3S,11aR)-N-((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
Company: ViiV Healthcare
Phase of Development: IIb
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Chemical Image:
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cabotegravir
cabotegravir
Molecular Weight: 405.3553
(Compound details obtained from ChemIDplus Advanced,1 NIAID Therapeutics Database,2 and ViiV Healthcare website3)
Patent Version Content

Pharmacology


Mechanism of Action: HIV-1 integrase strand transfer inhibitor. Cabotegravir (also known as S/GSK1265744) prevents viral DNA integration into the host genome and is being developed for both HIV treatment and prevention.4,5

Half-life (T½): 21 to 50 days (long-acting parenteral [LAP] nanosuspension administered via intramuscular [IM] or subcutaneous [SC] injection); 40 hours (oral dosing).6

Metabolism/Elimination: Cabotegravir is primarily metabolized via glucuronidation by UGT1A1 (main pathway) and UGT1A9 (minor pathway). Cytochrome P450 (CYP)-mediated metabolism is expected to have a minimal role in cabotegravir metabolism.7 Following a single oral radiolabeled dose of cabotegravir 30 mg, 58.5% of the administered dose was recovered in feces and 26.8% was recovered in urine. Cabotegravir is eliminated in feces primarily as unchanged drug and in urine as a glucuronide metabolite (M1).8

Resistance: In vitro, cabotegravir has exhibited activity against raltegravir-resistant isolates.9

Exposure of MT-2 cells infected with HIV-1 IIIB to increasing concentrations of cabotegravir for up to 112 days did not produce highly resistant mutants. Among 25 site-directed molecular clones containing single INSTI resistance substitutions, the majority remained fully susceptible to cabotegravir. However, the Q148K and Q148R mutants resulted in a moderate loss of efficacy for cabotegravir, with a 5.6-fold change (FC) with Q148K and a 5.1-FC with Q148R. Among 24 double or multiple integrase mutants, the following six had a FC >10 and were considered highly resistant to cabotegravir: E138A/Q148R, E138K/Q148K, E138K/Q148R, G140C/Q148R, G140S/Q148R, and Q148R/N155H. Cabotegravir cross-resistance to raltegravir and elvitegravir is limited. When tested against mutant viruses resistant to approved NRTIs, NNRTIs, and PIs, cabotegravir demonstrated efficacy with a potency similar to that against wild-type virus.10,11

In vitro analysis was performed on the susceptibility of recombinant viruses with patient-derived integrase from various clades of HIV-1 to cabotegravir. Fifty percent and 90% inhibitory concentrations (IC50 and IC90) of cabotegravir against each virus was comparable to cabotegravir’s activity against the wild-type control. No virus exhibited significant resistance to cabotegravir. Cabotegravir demonstrated a modest reduction in activity against two common integrase resistant viruses with the mutations G140S plus Q148H or E92Q plus N155H. These viruses, however, had significant resistance to raltegravir.12

In the Phase IIb LATTE study (NCT01641809), protocol-defined virologic failure was reported in seven total participants (three participants receiving oral CAB and four participants receiving efavirenz) during the 24-week induction phase of the study. During the induction phase, no treatment-emergent resistance was detected. During the 72-week maintenance phase of the study, five total participants experienced protocol-defined virologic failure: two in the CAB 10-mg group, one in the CAB 30-mg group, and two in the efavirenz group. Treatment-emergent resistance was detected in three participants, with two participants developing only NNRTI resistance mutations and one participant (who had low CAB and rilpivirine exposures) developing both an NNRTI (E138Q) and INI (Q148R) mutation.13

In the Phase IIb LATTE-2 study (NCT02120352), two participants (one participant in the every-8-weeks dosing group and one participant in the oral dosing group) met protocol-defined virologic failure during the maintenance phase of the study. There was no evidence of NRTI-, NNRTI-, or INI-resistance mutations at failure in either participant.14,15


Clinical Trials


Cabotegravir for HIV Treatment
Study Identifiers: LAI116482 (LATTE)16; NCT0164180917
Phase: IIb
Study Purpose: Dose-ranging efficacy study of oral CAB to select oral dose and evaluate oral CAB plus rilpivirine as a two-drug ART regimen for suppressive maintenance therapy
Study Population: HIV-infected, treatment–naive adults
Dosing:

  • Induction phase: Oral CAB 10, 30, or 60 mg once daily versus efavirenz 600 mg once daily, each given in combination with two background nucleoside reverse transcriptase inhibitors (NRTIs). The induction phase lasted through Week 24.
  • Maintenance phase: Those participants successfully completing the induction phase continued their randomized dose of oral CAB, but discontinued the background NRTIs and added rilpivirine 25 mg. The comparator arm continued with efavirenz 600 mg plus the background NRTIs. The maintenance phase lasted through Week 96.
  • Open-Label phase: Participants receiving oral CAB plus rilpivirine in the maintenance phase could enroll to continue treatment on the same regimen beyond Week 96.13,16-18

(See references cited above for information on study results.)

Study Identifier: LATTE-215; NCT0212035214
Phase: IIb
Study Purpose: Safety and efficacy study to (1) evaluate the antiviral activity, tolerability, and safety of two intramuscular (IM) dosing regimens of the long-acting injectables CAB LA plus rilpivirine LA (also known as TMC278 LA) relative to oral CAB plus abacavir/lamivudine (ABC/3TC) as maintenance therapy, and (2) select an IM regimen of CAB LA plus rilpivirine LA for progression into Phase III trials
Study Population: HIV-infected, treatment-naive adults
Dosing:

  • Induction phase: Once-daily regimen of oral CAB 30 mg plus ABC/3TC 600/300 mg for 20 weeks. In the last 4 weeks of the induction phase, participants also received oral rilpivirine 25 mg once daily. (Participants with HIV-1 RNA <50 copies/mL continued on to the maintenance phase of the study.)
  • Maintenance phase: Following induction, qualifying participants were randomized to one of the three treatment arms below for maintenance therapy. All doses of CAB LA and rilpivirine LA were given IM.
    • A loading dose of CAB LA 800 mg plus rilpivirine LA 600 mg were given on Day 1. Starting at Week 4, participants received a regimen of CAB LA 400 mg plus rilpivirine LA 600 mg, administered every 4 weeks until Week 32 (primary endpoint). Treatment will continue until Week 96 (or longer if continuing to extension phase).
    • A loading dose of CAB LA 800 mg plus rilpivirine LA 900 mg were given on Day 1. A second loading dose of CAB LA 600 mg was given at Week 4. Starting at Week 8, participants received a regimen of CAB LA 600 mg plus rilpivirine LA 900 mg, administered every 8 weeks until Week 32 (primary endpoint). Treatment will continue until Week 96 (or longer if continuing to extension phase).
    • Oral CAB 30 mg plus ABC/3TC administered daily until Week 32 (primary endpoint). Treatment will continue until Week 96 (or longer if electing to receive IM treatment during the extension phase).
  • Extension phase: For long-term collection of efficacy and safety data.

There will also be a long-term follow-up period for participants who withdraw from the study and have received at least one dose of CAB LA and/or rilpivirine LA.14,15,19,20

(See references cited above for information on study results.)

Cabotegravir for HIV Prevention
Study Identifier: ECLAIR; NCT0207617821
Phase: IIa
Study Purpose: Study to evaluate the safety, tolerability, and acceptability of CAB LA
Study Population: HIV-uninfected, adult males
Dosing:

  • Oral Phase: Participants initially received oral CAB 30 mg or placebo once daily for 4 weeks.
  • Injection Phase: Following a 1-week washout period, participants then received CAB LA 800 mg or placebo, administered by IM injection once every 12 weeks for 3 cycles.

Follow-up will continue for 40 weeks after the Week 41 primary endpoint.21-24

(See references cited above for information on study results.)

Another Phase IIa study (HPTN 077) will be evaluating the safety, tolerability, and pharmacokinetics of CAB LA in HIV-uninfected women and men.25 In addition, the Phase II CAPRISA 014 study will help to establish the safety and acceptability of CAB LA in at-risk HIV-uninfected women.26


Adverse Events


LATTE Study (NCT01641809)
In the Week 96 analysis of the LATTE study involving 243 treatment-naive participants (n = 181 CAB; n = 62 EFV), drug-related adverse events (AEs) ≥ Grade 2 occurred in 14% of participants in the oral CAB arm and in 19% of participants in the EFV arm, overall. Drug-related adverse events ≥ Grade 2 occurring during the 72-week maintenance phase were reported in 4% of oral CAB participants and 4% of EFV participants. Headache was more common with oral CAB treatment than with EFV treatment.

Serious adverse events (SAEs) occurred in 10% of participants receiving oral CAB and 6% of participants receiving EFV, with none of the SAEs in the oral CAB groups deemed drug-related and one of the SAEs in the EFV group considered drug-related. Three percent of oral CAB participants versus 15% of EFV participants withdrew from the study because of an AE (with most withdrawals occurring prior to the maintenance phase).

Grade 3-4 laboratory abnormalities occurred in 26% of participants assigned to oral CAB versus 37% of participants assigned to EFV, most commonly due to elevated CPK. Elevations in ALT (any grade) occurred in 20% of oral CAB participants and 21% of EFV participants.13,27

LATTE-2 Study (NCT02120352)
In the LATTE-2 study involving 309 participants, 286 participants were randomized to maintenance therapy (n = 115 IM CAB every 8 weeks; n = 115 IM CAB every 4 weeks; n = 56 oral CAB). Week 32 results found that the most common drug-related AE among participants receiving injectable medication was injection site pain, occurring in 92% of participants on IM medication. The most common injection site reactions (ISRs) reported during the maintenance phase overall were pain, swelling, and nodules. The majority of ISRs were mild or moderate in severity. Two participants (in the every-8-weeks dosing group) withdrew from the study because of an ISR.

The most common AEs not related to ISRs occurring in the injectable treatment groups were nasopharyngitis (20%), headache (14%), and diarrhea (12%). For participants in the oral treatment group, the most common AEs during the maintenance period were nasopharyngitis (25%), headache (7%), and diarrhea (5%).

Six percent of participants in the IM dosing groups and 5% of participants in the oral dosing group experienced an SAE during the maintenance phase, but none were drug-related. Nine participants withdrew from the study during the maintenance phase because of an AE.

Treatment-emergent lab abnormailites ≥ Grade 3 during the maintenance period occurred in 16% of participants in the IM dosing groups and in 14% of participants in the oral dosing group.15,19,20

ÉCLAIR Study (NCT02076178)
In the 41-week ECLAIR study involving a total of 126 treated participants (n = 105 CAB; n = 21 placebo), 18 participants withdrew from CAB during the study: 5 during oral therapy, 6 after oral therapy but prior to injections, and 7 during the injection period. During the injection phase, 4 out of 94 participants receiving CAB LA withdrew from the study because of injection intolerability. During the oral phase, 7 participants withdrew because of CAB-related AEs, which included three events of neutropenia, three events of increased blood CPK, and one event of fatigue.

Overall, Grade 2 to 4 AEs occurred in 62% of placebo participants and 80% of CAB participants. During the injection phase, 57% of participants in the placebo group experienced ISRs, whereas 93% of participants in the CAB LA group experienced ISRs. The majority of ISRs were Grade 1 or 2 in severity. The most common AE (Grade 2 to 4) for participants receiving CAB LA was injection site pain.

Grade 2 to 4 drug-related lab abnormalities occurred in 13% of CAB participants versus 5% of placebo participants. A majority of CAB LA participants reported satisfaction with side effects related to study medication. On items related to convenience, flexibility, and lifestyle, participants were more satisfied with CAB LA than with oral CAB.22-24

Meta-analysis
Safety data from eight Phase I or IIa clinical studies of oral CAB and CAB LA were evaluated in a meta-analysis. One hundred eighty-seven healthy and HIV-infected participants received oral CAB ranging from 5 mg to 50 mg for up to 14 days. Ninety-eight healthy participants received IM or SC CAB LA in single or repeat doses up to 800 mg.

No drug-related serious AEs occurred. The most common AEs not related to an ISR were headache (22%) and nausea (5%). ISRs related to CAB LA were predominately mild (93%) and Grade 1. No Grade 3 ISR AEs were reported. The most frequent ISRs related to the IM and SC long-acting injectables were pain (71% for IM; 24% for SC), erythema (9% for IM; 23% for SC), and nodules (7% for IM; 23% for SC). All ISRs were self-limited, and there were no study withdrawals because of an ISR.28


Drug Interactions


Oral CAB does not affect the pharmacokinetics of midazolam in human study participants, indicating that cabotegravir is neither a CYP inhibitor nor inducer. In vitro, cabotegravir does not inhibit UGT enzymes, except UGT1A3. (Cabotegraivr, however, is predicted to have no clinically significant effect on UGT1A3 substrates.) Cabotegravir does not inhibit hepatic, intestinal, or renal drug transporters, except for organic anion transporters 1 and 3 (OAT1/3). Drug-drug interactions are possible between cabotegravir and sensitive OAT1/3 substrates having a narrow therapeutic index (such as methotrexate).7,29

Co-administration of oral CAB with an oral contraceptive containing levonorgestrel (LNG) and ethinyl estradiol (EE) did not affect the pharmacokinetics of LNG or EE, suggesting oral CAB can be administered in combination with LNG- and EE-containing oral contraceptives without clinically significant interactions.30

There are no apparent pharmacokinetic interactions between oral CAB and etravirine or between oral CAB and rilpivirine.31,32


References


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  3. ViiV Healthcare website. Medicines in development. Available at: https://www.viivhealthcare.com/our-medicines/medicines-in-development.aspx. Last accessed on March 29, 2016.
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  7. Reese M, Ford S, Bowers G, et al. In vitro drug interaction profile of the HIV integrase inhibitor, GSK1265744, and demonstrated lack of clinical interaction with midazolam. Abstract presented at: 15th International Workshop on Clinical Pharmacology of HIV & Hepatitis Therapy; May 19-21, 2014; Washington, DC. Abstract P_20. Available at: http://regist2.virology-education.com/abstractbook/2014_4.pdf. Last accessed on March 29, 2016.
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Last Reviewed: March 29, 2016

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