Amendment: SEC Form SC 13G/A filed by Regulus Therapeutics Inc.

 UNITED STATES

SECURITIES AND EXCHANGE COMMISSION

Washington, D.C. 20549

SCHEDULE 13G

(Rule 13d-102)

INFORMATION TO BE INCLUDED IN STATEMENTS FILED PURSUANT

TO RULES 13d-1(b), (c), AND (d) AND AMENDMENTS THERETO FILED

PURSUANT TO RULE 13d-2(b)

(Amendment No. 7)¹

Check the appropriate box to designate the rule pursuant to which this Schedule is filed:

1              The remainder of this cover page shall be filled out for a reporting person’s initial filing on this form with respect to the subject class of securities, and for any subsequent amendment containing information which would alter disclosures provided in a prior cover page.

The information required on the remainder of this cover page shall not be deemed to be “filed” for the purpose of Section 18 of the Securities Exchange Act of 1934 (“Act”) or otherwise subject to the liabilities of that section of the Act but shall be subject to all other provisions of the Act (however, see the Notes).

(1) Consists of 312,671 Shares (defined in Item 2) issuable upon the exercise of A-2 Warrants (defined in Item 4) and 136,275 Shares issuable upon the exercise of A-3 Warrants (defined in Item 4).

(1) Consists of 312,671 Shares issuable upon the exercise of A-2 Warrants and 136,275 Shares issuable upon the exercise of A-3 Warrants.

(1) Consists of 263,545 Shares issuable upon the exercise of A-2 Warrants and 95,749 Shares issuable upon the exercise of A-3 Warrants.

(1) Consists of 263,545 Shares issuable upon the exercise of A-2 Warrants and 95,749 Shares issuable upon the exercise of A-3 Warrants.

(1) Consists of 43,419 Shares issuable upon the exercise of A-2 Warrants and 15,244 Shares issuable upon the exercise of A-3 Warrants.

(1) Consists of 43,419 Shares issuable upon the exercise of A-2 Warrants and 15,244 Shares issuable upon the exercise of A-3 Warrants.

(1) Consists of 576,216 Shares issuable upon the exercise of A-2 Warrants and 232,024 Shares issuable upon the exercise of A-3 Warrants.

(1) Consists of 630,628 Shares issuable upon the exercise of A-2 Warrants and 253,216 Shares issuable upon the exercise of A-3 Warrants.

(1) Consists of 630,628 Shares issuable upon the exercise of A-2 Warrants and 253,216 Shares issuable upon the exercise of A-3 Warrants.

(1) Consists of 630,628 Shares issuable upon the exercise of A-2 Warrants and 253,216 Shares issuable upon the exercise of A-3 Warrants.

Regulus Therapeutics Inc., a Delaware corporation (the “Issuer”).

4224 Campus Point Court, Suite 210

San Diego, California 92121

Biotechnology Value Fund, L.P. (“BVF”)

44 Montgomery St., 40th Floor

San Francisco, California 94104

Citizenship: Delaware

BVF I GP LLC (“BVF GP”)

44 Montgomery St., 40th Floor

San Francisco, California 94104

Citizenship: Delaware

Biotechnology Value Fund II, L.P. (“BVF2”)

44 Montgomery St., 40th Floor

San Francisco, California 94104

Citizenship: Delaware

BVF II GP LLC (“BVF2 GP”)

44 Montgomery St., 40th Floor

San Francisco, California 94104

Citizenship: Delaware

Biotechnology Value Trading Fund OS LP (“Trading Fund OS”)

PO Box 309 Ugland House

Grand Cayman, KY1-1104

Cayman Islands

Citizenship: Cayman Islands

BVF Partners OS Ltd. (“Partners OS”)

PO Box 309 Ugland House

Grand Cayman, KY1-1104

Cayman Islands

Citizenship: Cayman Islands

BVF GP Holdings LLC (“BVF GPH”)

44 Montgomery St., 40th Floor

San Francisco, California 94104

Citizenship: Delaware

BVF Partners L.P. (“Partners”)

44 Montgomery St., 40th Floor

San Francisco, California 94104

Citizenship: Delaware

BVF Inc.

44 Montgomery St., 40th Floor

San Francisco, California 94104

Citizenship: Delaware

Mark N. Lampert (“Mr. Lampert”)

44 Montgomery St., 40th Floor

San Francisco, California 94104

Citizenship: United States

Each of the foregoing is referred to as a “Reporting Person” and collectively as the “Reporting Persons.”

Common Stock, par value $0.001 per share (the “Shares”)

75915K309

As of the close of business on September 30, 2024, the Reporting Persons and a certain Partners managed account (the “Partners Managed Account”) held 630,628 A-2 Warrants (the “A-2 Warrants”) exercisable for an aggregate of 630,628 Shares. The A-2 Warrants are exercisable for a period of five years following the date of issuance and have an exercise price of $6.66 per Share. The A-2 Warrants may not be exercised if, after such exercise, the Reporting Persons would beneficially own, as determined in accordance with Section 13(d) of the Exchange Act, more than 9.99% of the number of Shares then issued and outstanding (the “A-2 Warrants Blocker”). As of the close of business on September 30, 2024, the A-2 Warrants Blocker did not limit the exercise of any of the A-2 Warrants held by the Reporting Persons and the Partners Managed Account.

As of the close of business on September 30, 2024, the Reporting Persons and the Partners Managed Account held 253,216 A-3 Warrants (the “A-3 Warrants”) exercisable for an aggregate of 253,216 Shares. The A-3 Warrants are exercisable for a period of five years following the date of issuance and have an exercise price of $7.464 per Share. The A-3 Warrants may not be exercised if, after such exercise, the Reporting Persons would beneficially own, as determined in accordance with Section 13(d) of the Exchange Act, more than 9.99% of the number of Shares then issued and outstanding (the “A-3 Warrants Blocker”). As of the close of business on September 30, 2024, the A-3 Warrants Blocker did not limit the exercise of any of the A-3 Warrants held by the Reporting Persons and the Partners Managed Account.

As of the close of business on September 30, 2024, (i) BVF beneficially owned 448,946 Shares, consisting of 312,671 Shares issuable upon the exercise of the A-2 Warrants held by it and 136,275 Shares issuable upon the exercise of the A-3 Warrants held by it; (ii) BVF2 beneficially owned 359,294 Shares, consisting of 263,545 Shares issuable upon the exercise of the A-2 Warrants held by it and 95,749 Shares issuable upon the exercise of the A-3 Warrants held by it; and (iii) Trading Fund OS beneficially owned 58,663 Shares, consisting of 43,419 Shares issuable upon the exercise of the A-2 Warrants held by it and 15,244 Shares issuable upon the exercise of the A-3 Warrants held by it.

BVF GP, as the general partner of BVF, may be deemed to beneficially own the 448,946 Shares beneficially owned by BVF.

BVF2 GP, as the general partner of BVF2, may be deemed to beneficially own the 359,294 Shares beneficially owned by BVF2.

Partners OS, as the general partner of Trading Fund OS, may be deemed to beneficially own the 58,663 Shares beneficially owned by Trading Fund OS.

BVF GPH, as the sole member of each of BVF GP and BVF2 GP, may be deemed to beneficially own the 808,240 Shares beneficially owned in the aggregate by BVF and BVF2.

Partners, as the investment manager of BVF, BVF2 and Trading Fund OS, and the sole member of Partners OS, may be deemed to beneficially own the 883,844 Shares beneficially owned in the aggregate by BVF, BVF2 and Trading Fund OS and held in the Partners Managed Account, including the 10,993 Shares issuable upon the exercise of A-2 Warrants held in the Partners Managed Account and 5,947 Shares issuable upon the exercise of the A-3 Warrants held in the Partners Managed Account.

BVF Inc., as the general partner of Partners, may be deemed to beneficially own the 883,844 Shares beneficially owned by Partners.

Mr. Lampert, as a director and officer of BVF Inc., may be deemed to beneficially own the 883,844 Shares beneficially owned by BVF Inc.

The foregoing should not be construed in and of itself as an admission by any Reporting Person as to beneficial ownership of any Shares owned by another Reporting Person. BVF GP disclaims beneficial ownership of the Shares beneficially owned by BVF. BVF2 GP disclaims beneficial ownership of the Shares beneficially owned by BVF2. Partners OS disclaims beneficial ownership of the Shares beneficially owned by Trading Fund OS. BVF GPH disclaims beneficial ownership of the Shares beneficially owned by BVF and BVF2. Each of Partners, BVF Inc. and Mr. Lampert disclaims beneficial ownership of the Shares beneficially owned by BVF, BVF2 and Trading Fund OS and held in the Partners Managed Account, and the filing of this statement shall not be construed as an admission that any such person or entity is the beneficial owner of any such securities.

The following percentages are based on a denominator that is the sum of (i) 65,465,876 Shares outstanding as of August 2, 2024 as set forth in the Issuer’s Quarterly Report on Form 10-Q filed with the Securities and Exchange Commission on August 8, 2024, (ii) 630,628 Shares issuable upon the exercise of A-2 Warrants and (iii) 253,216 Shares issuable upon the exercise of A-3 Warrants, as applicable.

As of the close of business on September 30, 2024, (i) BVF beneficially owned less than 1% of the outstanding Shares, (ii) BVF2 beneficially owned less than 1% of the outstanding Shares, (iii) Trading Fund OS beneficially owned less than 1% of the outstanding Shares, (iv) BVF GP may be deemed to beneficially own less than 1% of the outstanding Shares, (v) BVF2 GP may be deemed to beneficially own less than 1% of the outstanding Shares, (vi) Partners OS may be deemed to beneficially own less than 1% of the outstanding Shares, (vii) BVF GPH may be deemed to beneficially own approximately 1.2% of the outstanding Shares, and (viii) each of Partners, BVF Inc. and Mr. Lampert may be deemed to beneficially own approximately 1.3% of the outstanding Shares (less than 1% of the outstanding Shares are represented by Shares held in the Partners Managed Account).

See Cover Pages Items 5-9.

See Cover Pages Items 5-9.

See Cover Pages Items 5-9.

See Cover Pages Items 5-9.

If this statement is being filed to report the fact that as of the date hereof the Reporting Persons have ceased to be the beneficial owner of more than five percent of the Shares, check the following [X].

Not Applicable.

Not Applicable.

See Exhibit 99.1 to Amendment No. 4 to the Schedule 13G filed with the Securities and Exchange Commission on February 14, 2020.

Not Applicable.

By signing below each of the undersigned certifies that, to the best of its knowledge and belief, the securities referred to above were not acquired and are not held for the purpose of or with the effect of changing or influencing the control of the issuer of the securities and were not acquired and are not held in connection with or as a participant in any transaction having that purpose or effect.

SIGNATURE

After reasonable inquiry and to the best of his knowledge and belief, each of the undersigned certifies that the information set forth in this statement is true, complete and correct.

Dated: November 14, 2024